Furosemide(Synonyms: 呋塞米)

发表于2024年4月12日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Furosemide (Synonyms: 呋塞米) 纯度: 99.52%

Furosemide 是 Na⁺/K⁺/2Cl^– (NKCC)，NKCC1 和 NKCC2 共转运蛋白的有效的和具有口服活性抑制剂。Furosemide 也是 GABA_A 受体拮抗剂，对含 α6 受体的选择性是含 α1 受体的 100 倍。Furosemide 用作利尿试剂，用于充血性心力衰竭，高血压和水肿的研究。

Furosemide Chemical Structure

CAS No. : 54-31-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥500	In-stock
500 mg	￥400	In-stock
1 g	￥500	In-stock
5 g	￥1500	In-stock
10 g		询价
50 g		询价

* Please select Quantity before adding items.

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生物活性

Furosemide is a potent and orally active inhibitor of Na⁺/K⁺/2Cl^– (NKCC) cotransporter, NKCC1 and NKCC2^[1]. Furosemide is also a GABA_A receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema^[2].

IC₅₀ & Target

IC50: NKCC1 and NKCC2^[1]
IC50: GABA_A receptors^[2]

体外研究
(In Vitro)

Furosemide (500 µM; 72-96 hours) significantly changes the proliferation rates in MKN45 cells (the poorly differentiated human gastric adenocarcinoma cell line). however, it has no effects on MKN28 cells (the moderately differentiated human gastric adenocarcinoma cell line). The growth rate of MKN45 cells is larger than that of MKN28 cells^[4].
Furosemide (10 µM, 30 µM, 100 µM; 45 min exposure) significantly decreases cation channel activity and [Ca(2+)](i) in human erythrocytes drawn from healthy individuals. Tert-butylhydroperoxide similarly enhances the non-selective cation channels activity, increases [Ca(2+)](i) and triggered cell membrane scrambling, however, the effects is significantly blunted by furosemide again^[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Furosemide (intraperitoneal injection; 100 mg/kg; single dose) is injected after kanamycin (KM) (1000 mg/kg) to creat a deaf mouse model in C57BL/6 mouse. After injection, hearing loss and cochlear hair cell damage are evaluated on day 1, day 2 and day 3, respectively. The hearing is markedly deteriorated even from the next day (Day-1 group), OHCs (outer hair cell) morphology of apical, middle and basal turns are disorganized in mice on day3^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

330.74

Formula

C₁₂H₁₁ClN₂O₅S

CAS 号

54-31-9

中文名称

呋塞米；呋喃苯胺酸；速尿；利尿磺胺；速尿灵

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (302.35 mM)

H₂O : 0.1 mg/mL (0.30 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0235 mL	15.1176 mL	30.2352 mL
5 mM	0.6047 mL	3.0235 mL	6.0470 mL
10 mM	0.3024 mL	1.5118 mL	3.0235 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. C M Gillen, et al. Molecular cloning and functional expression of the K-Cl cotransporter from rabbit, rat, and human. A new member of the cation-chloride cotransporter family. J Biol Chem. 1996 Jul 5;271(27):16237-44.

[2]. S A Thompson, et al. Residues in transmembrane domains I and II determine gamma-aminobutyric acid type AA receptor subtype-selective antagonism by Furosemide sodium. Mol Pharmacol. 1999 Jun;55(6):993-9.

[3]. Shin Hye Kim, et al. Novel Peptide Vaccine GV1001 Rescues Hearing in Kanamycin/Furosemide sodium-Treated Mice. Front Cell Neurosci. 2018 Jan 19;12:3.

[4]. Atsushi Shiozaki , et al. Furosemide sodium, a blocker of Na+/K+/2Cl- cotransporter, diminishes proliferation of poorly differentiated human gastric cancer cells by affecting G0/G1 state. J Physiol Sci. 2006 Dec;56(6):401-6.

[5]. Yuliya V Kucherenko, et al.Inhibitory effect of Furosemide sodium on non-selective voltage-independent cation channels in human erythrocytes.Cell Physiol Biochem. 2012;30(4):863-75.

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SU4984

发表于2024年3月6日由上海金畔生物科技有限公司

SU4984 纯度: 99.94%

SU4984 是一种蛋白质酪氨酸激酶抑制剂，抑制成纤维细胞生长因子受体 1 (FGFR1) 的 IC₅₀ 值为 10-20 μM。SU4984 还可抑制血小板衍生的生长因子受体和胰岛素受体的活性。SU4984 可用于癌症研究。

SU4984 Chemical Structure

CAS No. : 186610-89-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
25 mg	￥2500	In-stock
50 mg	￥4500	In-stock
100 mg	￥7500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

SU4984 相关产品

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Anti-Liver Cancer Compound Library

生物活性

SU4984 is a protein tyrosine kinase inhibitor, with an IC₅₀ of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer^[1]^[2]^[3].

IC₅₀ & Target^[1]

FGFR1

10-20 μM (IC₅₀)

体外研究
(In Vitro)

SU4984 (5-100 μM; 5 min) inhibits the kinase activity of FGFR1K with an IC₅₀ of 10-20 μM in the presence of 1 mM adenosine triphosphate (ATP)^[1].
SU4984 (10-90 μM; 5 min) inhibits the autophosphorylation of FGFR1 induced by aFGF in NIH 3T3 cells, with an IC₅₀ of 20-40 μM^[1].
SU4984 (5 μM) substantially reduces tyrosine phosphorylation of the wild-type receptor and reduces 50% phosphorylation of constitutive C2 KIT^[2].
SU4984 (1-10 μM; 6 days) kills the C2 and P815 cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

333.38

Formula

C₂₀H₁₉N₃O₂

CAS 号

186610-89-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 50 mg/mL (149.98 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9996 mL	14.9979 mL	29.9958 mL
5 mM	0.5999 mL	2.9996 mL	5.9992 mL
10 mM	0.3000 mL	1.4998 mL	2.9996 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (15.00 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (15.00 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Mohammadi M, et, al. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997 May 9;276(5314):955-60.

[2]. Ma Y, et, al. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4.

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ELN-441958

发表于2024年3月5日由上海金畔生物科技有限公司

ELN-441958 纯度: 99.84%

ELN-441958是有效的B1受体拮抗剂, 抑制B1激动剂配体[3H] DAKD与IMR-90细胞结合, Ki值为 0.26 nM, ELN-441958抑制B1受体比作抑制 B2受体具有更高的选择性, 比抑制μ/δ阿片受体选择性分别高500和2000多倍。

ELN-441958 Chemical Structure

CAS No. : 913064-47-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3858	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg	￥15000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

ELN-441958 相关产品

•相关化合物库:

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生物活性

ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor. IC50 value: 0.26 nM (Ki) Target: B1 Receptor in vitro: ELN-441958 is a novel small molecule bradykinin B1 receptor antagonist, based on the inhibition of agonist-induced increases in intracellular calcium in native and recombinant cells. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. ELN-441958 also displays good selectivity for B1 over other receptors examined in a broad screening panel. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptor, the most potent off-target activity identified. In IMR-90 cells expressing the native human B1 receptor, ELN-441958 produced a concentration-dependent antagonism of the DAKD-induced calcium mobilization with a KB of 0.12 nM. [1] in vivo: ELN-441958 is essentially completely absorbed and produces high plasma levels after oral administration in rhesus monkeys.ELN-441958 has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes. ELN-441958 has high oral exposure and moderate plasma half-lives in rats and rhesus monkeys. The oral availability of ELN441958 in rats was 57%. ELN-441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 3 mg/kg s.c. [1]

分子量

501.02

Formula

C₂₉H₂₉ClN₄O₂

CAS 号

913064-47-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (199.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9959 mL	9.9796 mL	19.9593 mL
5 mM	0.3992 mL	1.9959 mL	3.9919 mL
10 mM	0.1996 mL	0.9980 mL	1.9959 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Hawkinson JE, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther.2007 Aug;322(2):619-630.

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L748337

发表于2024年2月23日由上海金畔生物科技有限公司

L748337 纯度: 96.41%

L748337 是一种有效的 β3-肾上腺素能受体 (β3-adrenergic receptor) 拮抗剂，对 β1 和 β2 受体具有选择性。L748337 对 β3-、β2- 和 β1-肾上腺素受体的 K_i 值分别为 4.0 nM、204 nM 和 390 nM。L748337 主要与 G_i 结合激活 MAPK 信号并增加 Erk1/2 的磷酸化，其 pEC₅₀ 值为 11.6。L748337 可用于癌症、非酒精性脂肪性肝病 (NAFLD) 及心血管相关等疾病的研究。

L748337 Chemical Structure

CAS No. : 244192-94-7

规格	价格	是否有货
5 mg	￥5300	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

L748337 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The K_i values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively^[1]. L748337 couples predominantly to G_i to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC₅₀ value of 11.6^[2]. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases^[1]^[2]^[3].

IC₅₀ & Target^[1]

Beta-3 adrenergic receptor

4 nM (Ki)

Beta-2 adrenergic receptor

204 nM (Ki)

Beta-1 adrenergic receptor

390 nM (Ki)

体外研究
(In Vitro)

L748337 (1 μM) inhibits iNOS expression in B16F10 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

L-748337 (intraperitoneal injection; 5 mg/kg; beginning 10 days until D18) decreases the growth of melanoma induced by B16F10 cell inoculation and decreases tumor vasculature in mice^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Fifty male C57BL/6 J mice (8 weeks of age) bearing syngeneic B16F10 cell^[1]
Dosage:	5 mg/kg
Administration:	Beginning 10 days until D18
Result:	Exhibited anti-cancer effects.

分子量

497.61

Formula

C₂₆H₃₁N₃O₅S

CAS 号

244192-94-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

Ethanol : 30 mg/mL (60.29 mM; Need ultrasonic and warming)

DMSO : 25 mg/mL (50.24 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0096 mL	10.0480 mL	20.0961 mL
5 mM	0.4019 mL	2.0096 mL	4.0192 mL
10 mM	0.2010 mL	1.0048 mL	2.0096 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. S Neidhold, et al. The function of alpha- and beta-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br J Pharmacol. 2007 Feb;150(3):261-70.

[2]. Masaaki Sato, et al. The beta3-adrenoceptor agonist 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-phenyl]-benzenesulfonamide (L755507) and antagonist (S)-N-[4-[2-[[3-[3-(acetamidomethyl)phenoxy]-2-hydroxypropyl]amino]-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1 cells stably expressing the human beta3-adrenoceptor. Mol Pharmacol. 2008 Nov;74(5):1417-28.

[3]. Ziwen Wang, et al. The protective effects of the β3 adrenergic receptor agonist BRL37344 against liver steatosis and inflammation in a rat model of high-fat diet-induced nonalcoholic fatty liver disease (NAFLD). Mol Med. 2020 Jun 5;26(1):54.

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PB28 dihydrochloride

发表于2024年2月22日由上海金畔生物科技有限公司

PB28 dihydrochloride 纯度: 99.53%

PB28 dihydrochloride，一种环己基哌嗪衍生物，是一种 K_i 值为 0.68 nM 的高亲和力和选择性 sigma 2 (σ2) 受体激动剂。PB28 dihydrochloride 也是一种 σ1 受体拮抗剂，K_i 为 0.38 nM，对其他受体的亲和力较小。PB28 dihydrochloride 抑制豚鼠膀胱和回肠中的电诱发抽搐，其 EC₅₀ 值分别为 2.62 μM 和 3.96 μM。PB28 dihydrochloride 可以调节 SARS-CoV-2-人之间的蛋白质与蛋白质的相互作用。PB28 dihydrochloride 可诱导非 caspase 依赖性的细胞凋亡 (apoptosis)，并具有抗肿瘤活性。

PB28 dihydrochloride Chemical Structure

CAS No. : 172907-03-8

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10 mg	￥4800	In-stock
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100 mg		询价

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GPCR/G Protein Compound Library
Neuronal Signaling Compound Library
Anti-Cancer Compound Library
Antiviral Compound Library

生物活性

PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity^[1]^[2]^[3]^[4]^[5].

体外研究
(In Vitro)

PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) dihydrochloride treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent^[1].
PB28 dihydrochloride has a higher σ2 receptor affinity expressed as K_i (0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively)^[1].
PB28 dihydrochloride inhibits cell growth of MCF7 and MCF7 ADR cells with IC₅₀s of 25 nM and 15 nM, respectively after 2-day treatment^[1].
PB28 dihydrochloride induces apoptosis through a caspase-independent pathway^[1].
PB28 dihydrochloride also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR)^[1].
PB28 dihydrochloride displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	MCF7 and MCF7 ADR cells
Concentration:	25 nM and 15 nM
Incubation Time:	24 hours, 48 hours
Result:	Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

体内研究
(In Vivo)

PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) dihydrochloride treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 female mice (10 weeks old) injected with Panc02 cells^[2]
Dosage:	10.7 mg/mL
Administration:	Intraperitoneal injection; daily; for two weeks
Result:	Inhibited tumor growth in Panc02 tumor burden mice.

分子量

443.49

Formula

C₂₄H₄₀Cl₂N₂O

CAS 号

172907-03-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 10 mg/mL (22.55 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2548 mL	11.2742 mL	22.5484 mL
5 mM	0.4510 mL	2.2548 mL	4.5097 mL
10 mM	0.2255 mL	1.1274 mL	2.2548 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5(7):1807-16.

[2]. Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. BMC Cancer. 2017 Jan 13;17(1):51.

[3]. Nicola A Colabufo, et al. A New Method for Evaluating sigma(2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368(2):106-12.

[4]. Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). J Med Chem. 2009 Dec 10;52(23):7817-28.

[5]. David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386.

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CITCO

发表于2024年2月21日由上海金畔生物科技有限公司

CITCO 纯度: 99.17%

CITCO 是一种组成型雄甾烷 (Constitutive androstane) 受体激动剂，抑制脑肿瘤干细胞 (BTSCs) 的生长和扩增。CITCO 是一种咪唑并噻唑衍生物，其作为人 CAR 的选择性激动剂起作用。CITCO 对于孕烷 X 受体 (PXR) 的 EC₅₀ 为 49 nM，并且对其他核受体没有活性。

CITCO Chemical Structure

CAS No. : 338404-52-7

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1845	In-stock
5 mg	￥1675	In-stock
10 mg	￥2680	In-stock
25 mg	￥5360	In-stock
50 mg	￥8580	In-stock
100 mg		询价
200 mg		询价

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CITCO 相关产品

•相关化合物库:

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生物活性

CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC₅₀ of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors^[1].

IC₅₀ & Target

CAR, PXR^[1]

体外研究
(In Vitro)

CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs^[1].
CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes^[1].
CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes^[1].
CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes
Concentration:	1, 2.5, 5, 10, 25, 50 μM
Incubation Time:	48 hours
Result:	Resulted in a dose-dependent inhibition of viable cell count and proliferation.

Cell Cycle Analysis^[1]

Cell Line:	The T98G, U87MG, DB29 and DB33 glioma cells
Concentration:	2.5, 5 μM
Incubation Time:	48 hours
Result:	Induced cell cycle arrest differentially in different BTSCs in culture.

Apoptosis Analysis^[1]

Cell Line:	The T98G, U87MG, DB29 and DB33 glioma cells
Concentration:	2.5, 5 or 10 μM
Incubation Time:	48 hours
Result:	Increased the levels of Annexin V-positive apoptotic cells in dose dependently.

Western Blot Analysis^[1]

Cell Line:	T98G, U87MG, DB29 and DB33 glioma cells
Concentration:	0 to 25 μM
Incubation Time:	48 hours
Result:	The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.

体内研究
(In Vivo)

CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO ^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six- to eight-week-old male athymic nude mice^[1]
Dosage:	25 or 100 μg
Administration:	Intraperitoneal; on days 22, 24, 26, 30 and 36
Result:	Decreased tumour growth.

分子量

436.74

Formula

C₁₉H₁₂Cl₃N₃OS

CAS 号

338404-52-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 25 mg/mL (57.24 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2897 mL	11.4485 mL	22.8969 mL
5 mM	0.4579 mL	2.2897 mL	4.5794 mL
10 mM	0.2290 mL	1.1448 mL	2.2897 mL

参考文献

[1]. Chakraborty S, et al. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. Br J Cancer. 2011 Feb 1;104(3):448-59.

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BA 1 TFA

发表于2024年2月16日由上海金畔生物科技有限公司

BA 1 TFA 纯度: 99.65%

BA 1 TFA 是一种 bombesin (BB) 受体家族激动剂。BA 1 与 Bombesin 受体亚型 3 (BRS3)，胃泌素释放肽受体 (GRPR)，神经调节素 B 受体 (NMBR) 高亲和力结合，IC₅₀ 分别为 6、0.4、2.5 nM 。

BA 1 TFA Chemical Structure

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5 mg	￥2000	In-stock
10 mg		询价
50 mg		询价

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Peptide Library

生物活性

BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC₅₀s of 6, 0.4, 2.5 nM^[1].

体外研究
(In Vitro)

BA1 (0.1 μM) significantly increases FAK tyrosine phosphorylation in BRS-3 transfected NCI-H1299 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1247.32

Formula

C₅₉H₇₇F₃N₁₄O₁₃

Sequence Shortening

YQWAV{Bal}HF{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

参考文献

[1]. Terry W Moody, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.

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PU02

发表于2024年2月16日由上海金畔生物科技有限公司

PU02 纯度: 99.29%

PU02 是 6-MP (HY-13677) 的一个衍生物，是 5-HT₃ 受体的负变构调节剂，其在 HEK293 细胞测得的转染 5-HT₃A 和 5-HT₃AB 受体后的 IC₅₀ 值分别为 0.36 和 0.73 μM。

PU02 Chemical Structure

CAS No. : 313984-77-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥940	In-stock
10 mg	￥850	In-stock
50 mg	￥3000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

PU02 相关产品

•相关化合物库:

Bioactive Compound Library Plus
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GPCR/G Protein Compound Library
Neuronal Signaling Compound Library
Anti-Cancer Compound Library
Neurotransmitter Receptor Compound Library
Anti-Alzheimer’s Disease Compound Library
Anti-Parkinson’s Disease Compound Library
Neurodegenerative Disease-related Compound Library

生物活性

PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT₃ receptor, with IC₅₀ values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT₃A and 5-HT₃AB receptors respectively^[1]^[2].

IC₅₀ & Target^[1]

5-HT_3A Receptor

0.36 μM (IC₅₀)

5-HT ₃ AB

0.73 μM (IC₅₀)

体外研究
(In Vitro)

PU02 (NMMP) (0-200 μM) leads to a steady decrease in cell viability of HepG2 cells (IC₅₀=48.585 μM). PU02 (NMMP) shows less toxicity on L02 cells than did 6-MP after 48 h of treatment^[2].
PU02 (NMMP) at 6.25 or 25 μM exhibits inhibitory effects on the viability of the tested cell lines, including SMMC-7721, MDA-MB-231, RKO and HCT-8 cells^[2].
PU02 (NMMP) induces cell cycle arrest at the G2/M phase. PU02 (NMMP) downregulats the expression of cyclin B1/D1 and CDK4 in a time-dependent manner in HepG2 cells,but the expression of cyclin E is not affected^[2].
PU02 (NMMP)-treated cells exhibits a significant increase in caspase-3 cleavage, suggesting enhanced apoptotic activity^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[2]

Cell Line:	HepG2 cells.
Concentration:	6.26, 12.5, 25, 50 μM.
Incubation Time:	6, 12, 24, 36 h.
Result:	Induced mitochondria-dependent apoptosis.

分子量

292.36

Formula

C₁₆H₁₂N₄S

CAS 号

313984-77-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (855.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4204 mL	17.1022 mL	34.2044 mL
5 mM	0.6841 mL	3.4204 mL	6.8409 mL
10 mM	0.3420 mL	1.7102 mL	3.4204 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.11 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.11 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Sarah M Trattnig, et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54.

[2]. Xiao-Guang Yang, et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2012 Nov 15;695(1-3):27-33.

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PB28

发表于2024年1月29日由上海金畔生物科技有限公司

PB28

PB28 是一种环己基哌嗪衍生物，是一种 K_i 值为 0.68 nM 的高亲和力和选择性 sigma 2 (σ2) 受体激动剂。PB28 也是一种 σ1 受体拮抗剂，K_i 为 0.38 nM，对其他受体的亲和力较小。PB28 抑制豚鼠膀胱和回肠中的电诱发抽搐，其 EC₅₀ 值分别为 2.62 μM 和 3.96 μM。PB28 可以调节 SARS-CoV-2-人之间的蛋白质与蛋白质的相互作用。PB28 可诱导非 caspase 依赖性的细胞凋亡 (apoptosis)，并具有抗肿瘤活性。

PB28 Chemical Structure

CAS No. : 172906-90-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

PB28 的其他形式现货产品:

PB28 dihydrochloride

生物活性

PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 is also a σ1 antagonist with a K_i of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)^[4]

体外研究
(In Vitro)

PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent^[1].
PB28 has a higher σ2 receptor affinity expressed as K_i (0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively)^[1].
PB28 inhibits cell growth of MCF7 and MCF7 ADR cells with IC₅₀s of 25 nM and 15 nM, respectively after 2-day treatment^[1].
PB28 induces apoptosis through a caspase-independent pathway^[1].
PB28 also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR)^[1].
PB28 displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	MCF7 and MCF7 ADR cells
Concentration:	25 nM and 15 nM
Incubation Time:	24 hours, 48 hours
Result:	Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

体内研究
(In Vivo)

PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 female mice (10 weeks old) injected with Panc02 cells^[2]
Dosage:	10.7 mg/mL
Administration:	Intraperitoneal injection; daily; for two weeks
Result:	Inhibited tumor growth in Panc02 tumor burden mice.

分子量

370.57

Formula

C₂₄H₃₈N₂O

CAS 号

172906-90-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5(7):1807-16.

[2]. Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. BMC Cancer. 2017 Jan 13;17(1):51.

[3]. Nicola A Colabufo, et al. A New Method for Evaluating sigma(2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368(2):106-12.

[4]. Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). J Med Chem. 2009 Dec 10;52(23):7817-28.

[5]. David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BA 1

发表于2024年1月29日由上海金畔生物科技有限公司

BA 1

BA 1 是一种 bombesin (BB) 受体家族激动剂。BA 1 与 Bombesin 受体亚型 3 (BRS3)，胃泌素释放肽受体 (GRPR)，神经调节素 B 受体 (NMBR) 高亲和力结合，IC₅₀ 分别为 6、0.4、2.5 nM 。

BA 1 Chemical Structure

CAS No. : 183241-31-8

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BA 1 的其他形式现货产品:

BA 1 TFA

生物活性

BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC₅₀s of 6, 0.4, 2.5 nM^[1].

体外研究
(In Vitro)

BA 1 (0.1 μM) significantly increases FAK tyrosine phosphorylation in BRS-3 transfected NCI-H1299 cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1133.30

Formula

C₉H₁₉FN₃O₂VWY

CAS 号

183241-31-8

Sequence Shortening

YQWAV{Bal}HF{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

参考文献

[1]. Terry W Moody, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PB28

发表于2024年1月29日由上海金畔生物科技有限公司

PB28

PB28 Chemical Structure

CAS No. : 172906-90-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

PB28 的其他形式现货产品:

PB28 dihydrochloride

生物活性

IC₅₀ & Target

Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)^[4]

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	MCF7 and MCF7 ADR cells
Concentration:	25 nM and 15 nM
Incubation Time:	24 hours, 48 hours
Result:	Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 female mice (10 weeks old) injected with Panc02 cells^[2]
Dosage:	10.7 mg/mL
Administration:	Intraperitoneal injection; daily; for two weeks
Result:	Inhibited tumor growth in Panc02 tumor burden mice.

分子量

370.57

Formula

C₂₄H₃₈N₂O

CAS 号

172906-90-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5(7):1807-16.

[2]. Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. BMC Cancer. 2017 Jan 13;17(1):51.

[3]. Nicola A Colabufo, et al. A New Method for Evaluating sigma(2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368(2):106-12.

[4]. Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). J Med Chem. 2009 Dec 10;52(23):7817-28.

[5]. David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BA 1

发表于2024年1月29日由上海金畔生物科技有限公司

BA 1

BA 1 Chemical Structure

CAS No. : 183241-31-8

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BA 1 的其他形式现货产品:

BA 1 TFA

生物活性

体外研究
(In Vitro)

BA 1 (0.1 μM) significantly increases FAK tyrosine phosphorylation in BRS-3 transfected NCI-H1299 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1133.30

Formula

C₉H₁₉FN₃O₂VWY

CAS 号

183241-31-8

Sequence Shortening

YQWAV{Bal}HF{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

参考文献

[1]. Terry W Moody, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PB28

发表于2024年1月29日由上海金畔生物科技有限公司

PB28

PB28 Chemical Structure

CAS No. : 172906-90-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

PB28 的其他形式现货产品:

PB28 dihydrochloride

生物活性

IC₅₀ & Target

Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)^[4]

体外研究
(In Vitro)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	MCF7 and MCF7 ADR cells
Concentration:	25 nM and 15 nM
Incubation Time:	24 hours, 48 hours
Result:	Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 female mice (10 weeks old) injected with Panc02 cells^[2]
Dosage:	10.7 mg/mL
Administration:	Intraperitoneal injection; daily; for two weeks
Result:	Inhibited tumor growth in Panc02 tumor burden mice.

分子量

370.57

Formula

C₂₄H₃₈N₂O

CAS 号

172906-90-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5(7):1807-16.

[2]. Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. BMC Cancer. 2017 Jan 13;17(1):51.

[3]. Nicola A Colabufo, et al. A New Method for Evaluating sigma(2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368(2):106-12.

[4]. Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). J Med Chem. 2009 Dec 10;52(23):7817-28.

[5]. David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BA 1

发表于2024年1月29日由上海金畔生物科技有限公司

BA 1

BA 1 Chemical Structure

CAS No. : 183241-31-8

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BA 1 的其他形式现货产品:

BA 1 TFA

生物活性

体外研究
(In Vitro)

BA 1 (0.1 μM) significantly increases FAK tyrosine phosphorylation in BRS-3 transfected NCI-H1299 cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1133.30

Formula

C₉H₁₉FN₃O₂VWY

CAS 号

183241-31-8

Sequence Shortening

YQWAV{Bal}HF{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

参考文献

[1]. Terry W Moody, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Siramesine(Synonyms: Lu 28-179)

发表于2023年11月15日由上海金畔生物科技有限公司

Siramesine (Synonyms: Lu 28-179)

Siramesine (Lu 28-179) 是一种有效的 sigma-2 受体激动剂。Siramesine 对 sigma-2 受体具有亚纳摩尔亲和力 (IC₅₀=0.12 nM)，并且对 sigma-2 受体的选择性是 sigma-1 受体的 140倍 (IC₅₀=17 nM)。Siramesine 通过线粒体的不稳定而不是溶酶体触发细胞死亡。Siramesine 显示出强大的抗癌活性。

Siramesine Chemical Structure

CAS No. : 147817-50-3

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Siramesine 的其他形式现货产品:

Siramesine hydrochloride

生物活性	Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity^[1]^[2]^[3].
体外研究 (In Vitro)	Siramesine displays the binding affinities: IC₅₀ (sigma 1)=17 nM, IC₅₀ (sigma 2)=0.12 nM, IC₅₀ (5-HT_1A)=21000 nM, IC₅₀ (5-HT_1A)=2000 nM, IC₅₀ (D₂)=800 nM, IC₅₀ (alpha 1)=330 nM^[1]. Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)^[2]. Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells^[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	454.58
Formula	C₃₀H₃₁FN₂O
CAS 号	147817-50-3
中文名称	西拉美新
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008. [2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3. [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Siramesine(Synonyms: Lu 28-179)

发表于2023年11月15日由上海金畔生物科技有限公司

Siramesine (Synonyms: Lu 28-179)

Siramesine Chemical Structure

CAS No. : 147817-50-3

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Siramesine 的其他形式现货产品:

Siramesine hydrochloride

生物活性	Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity^[1]^[2]^[3].
体外研究 (In Vitro)	Siramesine displays the binding affinities: IC₅₀ (sigma 1)=17 nM, IC₅₀ (sigma 2)=0.12 nM, IC₅₀ (5-HT_1A)=21000 nM, IC₅₀ (5-HT_1A)=2000 nM, IC₅₀ (D₂)=800 nM, IC₅₀ (alpha 1)=330 nM^[1]. Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)^[2]. Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	454.58
Formula	C₃₀H₃₁FN₂O
CAS 号	147817-50-3
中文名称	西拉美新
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008. [2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3. [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Siramesine(Synonyms: Lu 28-179)

发表于2023年11月15日由上海金畔生物科技有限公司

Siramesine (Synonyms: Lu 28-179)

Siramesine Chemical Structure

CAS No. : 147817-50-3

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Siramesine 的其他形式现货产品:

Siramesine hydrochloride

生物活性	Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity^[1]^[2]^[3].
体外研究 (In Vitro)	Siramesine displays the binding affinities: IC₅₀ (sigma 1)=17 nM, IC₅₀ (sigma 2)=0.12 nM, IC₅₀ (5-HT_1A)=21000 nM, IC₅₀ (5-HT_1A)=2000 nM, IC₅₀ (D₂)=800 nM, IC₅₀ (alpha 1)=330 nM^[1]. Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)^[2]. Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells^[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	454.58
Formula	C₃₀H₃₁FN₂O
CAS 号	147817-50-3
中文名称	西拉美新
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008. [2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3. [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499.

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Regadenoson(Synonyms: 瑞加德松; CVT-3146)

发表于2023年11月3日由上海金畔生物科技有限公司

Regadenoson (Synonyms: 瑞加德松; CVT-3146) 纯度: 99.59%

Regadenoson (CVT-3146) 是一种有效的选择性 A2A 腺苷受体激动剂，对大鼠和猪腺苷 A2A 受体的 K_i 分别为 290 和 1120 nM。Regadenoson 对 A2A 受体的选择性高于人 A1 和 A2B 受体，其选择性是 A1 受体的 13 倍。Regadenoson 是一种血管扩张剂，它改变了血管扩张剂心肌灌注显像的前景。Regadenoson 增加了啮齿动物血脑屏障 (BBB) 的通透性。

Regadenoson Chemical Structure

CAS No. : 313348-27-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥850	In-stock
2 mg	￥600	In-stock
5 mg	￥990	In-stock
10 mg	￥1700	In-stock
25 mg	￥3100	In-stock
50 mg	￥4650	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

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生物活性

Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with K_is of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents^[1]^[2]^[3].

Clinical Trial

分子量

390.35

Formula

C₁₅H₁₈N₈O₅

CAS 号

313348-27-5

中文名称

瑞加德松；类伽腺苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (128.09 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5618 mL	12.8090 mL	25.6180 mL
5 mM	0.5124 mL	2.5618 mL	5.1236 mL
10 mM	0.2562 mL	1.2809 mL	2.5618 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Palle VP, et al. Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor. Bioorg Med Chem Lett. 2002;12(20):2935-2939.

[2]. Golzar Y, et al. Regadenoson use in patients with chronic obstructive pulmonary disease: the state of current knowledge. Int J Chron Obstruct Pulmon Dis. 2014;9:129-137. Published 2014 Jan 22.

[3]. Jackson S, et al. The effect of regadenoson on the integrity of the human blood-brain barrier, a pilot study. J Neurooncol. 2017;132(3):513-519.

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Lenvatinib(Synonyms: 仑伐替尼; E7080)

发表于2023年11月2日由上海金畔生物科技有限公司

Lenvatinib (Synonyms: 仑伐替尼; E7080) 纯度: 99.87%

Lenvatinib (E7080) 一种具有口服活性的，多靶点酪氨酸激酶抑制剂，抑制血管内皮生长因子受体 (VEGFR1-3)，成纤维细胞生长因子受体 (FGFR1-4)，血小板衍生生长因子受体 (PDGFR)，干细胞因子受体 (KIT)，转染期间重排 (RET)，显示有效抗癌的活性。

Lenvatinib Chemical Structure

CAS No. : 417716-92-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥798	In-stock
2 mg	￥520	In-stock
5 mg	￥850	In-stock
10 mg	￥1200	In-stock
50 mg	￥4500	In-stock
100 mg	￥7500	In-stock
200 mg	￥12000	In-stock
500 mg	￥24000	In-stock
1 g		询价
5 g		询价

* Please select Quantity before adding items.

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生物活性

Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities^[1]^[2].

IC₅₀ & Target^[1]^[2]^[3]

VEGFR2

4 nM (IC₅₀)

VEGFR3

5.2 nM (IC₅₀)

VEGFR1

22 nM (IC₅₀)

FGFR1

46 nM (IC₅₀)

FGFR2

FGFR3

FGFR4

PDGFRα

51 nM (IC₅₀)

PDGFRβ

39 nM (IC₅₀)

c-Kit

100 nM (IC₅₀)

RET

体外研究
(In Vitro)

Lenvatinib (E7080) has IC₅₀s of 4, 5.2, 22 nM for VEGFR2 (KDR), VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC₅₀s of 51, 39, 46, and 100 nM, respectively^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Lenvatinib (E7080) (100 mg/kg, p.o.) significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung^[3].
Lenvatinib (E7080) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and STI571 treatment^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

426.85

Formula

C₂₁H₁₉ClN₄O₄

CAS 号

417716-92-8

中文名称

乐伐替尼；仑伐替尼；乐法替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 12.78 mg/mL (29.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3427 mL	11.7137 mL	23.4274 mL
5 mM	0.4685 mL	2.3427 mL	4.6855 mL
10 mM	0.2343 mL	1.1714 mL	2.3427 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 0.5% Methylcellulose/saline water

Solubility: 6.67 mg/mL (15.63 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.86 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.86 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.86 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
5.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 0.64 mg/mL (1.50 mM); Clear solution

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Kudo M, et al. Lenvatinib versus Bay 43-9006 in first-line treatment of patients with unresectable hepatocellularcarcinoma: a randomised phase 3 non-inferiority trial. Lancet. 2018 Mar 24;391(10126):1163-1173.

[2]. Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361.

[3]. Matsui J, et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008, 122(3), 664-671.

[4]. Matsui J, et al. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res. 2008, 14(17),545.

Cell Assay ^[1]	H146 (1.2×10³ cells/50 μL/well) in SFM containing 0.5% BSA are cultured in 96-well multi-plates. After overnight culture at 37°C, SFM (150 μL/well) containing 0.5% FBS and several concentrations of SCF are added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells are measured by WST-1. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Female BALB/c nude mice (8-12 weeks old, 20-25 g) are maintained under clean-room conditions. H146 tumor cells (6.5×10⁶) are implanted subcutaneously (s.c.) into the flank region of mice. Twelve days after inoculation, mice are randomized into control (n=12) and treatment (n=6 or n=5) groups and this point in time is identified as day 1. Lenvatinib and STI571, and VEGF neutralization antibody are suspended in 0.5% methylcellulose and saline, respectively, and administered orally twice a day for lenvatinib and STI571 and twice a week for antibody from day 1 to day 21. Tumor volume is measured on the indicated days and calculated. Antitumor activity is shown as a relative tumor volume (RTV=calculated tumor volume at indicated days/volume on day 1). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Kudo M, et al. Lenvatinib versus Bay 43-9006 in first-line treatment of patients with unresectable hepatocellularcarcinoma: a randomised phase 3 non-inferiority trial. Lancet. 2018 Mar 24;391(10126):1163-1173. [2]. Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361. [3]. Matsui J, et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008, 122(3), 664-671. [4]. Matsui J, et al. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res. 2008, 14(17),545.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SCH 58261

发表于2023年8月25日由上海金畔生物科技有限公司

SCH 58261 纯度: 99.78%

SCH 58261 是一种强效、选择性的竞争性腺苷 A2A 受体拮抗剂，IC₅₀ 值为 15 nM，对 A2A 受体的选择性分别是 A1、A2B 和 A3 受体的 323 倍、53 倍、100 倍。

SCH 58261 Chemical Structure

CAS No. : 160098-96-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥858	In-stock
5 mg	￥780	In-stock
10 mg	￥1550	In-stock
50 mg	￥5900	In-stock
100 mg	￥9950	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

SCH 58261 相关产品

•相关化合物库:

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Neurodegenerative Disease-related Compound Library

生物活性

SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC₅₀ of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively^[1]^[2]^[3].

IC₅₀ & Target

IC50: 15 nM (A2A receptor)^[2]

体外研究
(In Vitro)

SCH 58261 (0 nM–10 µM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975^[4].
SCH58261 (25 μM; 72 hours) can inhibit the growth of CAF cells^[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[4]

Cell Line:	H1975 cells
Concentration:	10 nM-10 µM
Incubation Time:	7 days
Result:	Produced a concentration-dependent decrease in H1975 cell growth.

Cell Proliferation Assay^[5]

Cell Line:	CAF cells
Concentration:	25 μM
Incubation Time:	72 hours
Result:	Inhibit the growth of CAF1 and CAF2 cells.

体内研究
(In Vivo)

SCH 58261 (2 mg/kg; i.p.; daily; for 20 days) causes a decrease in the tumor burden in a NSCLC mouse model^[5].
SCH 58261 (5 mg/kg; i.p.; 3 times; every 3 hours; 10 minutes before haloperidol) partially decreases the haloperidol-induced catalepsy and the increase in the PENK mRNA expression in both dorsolateral and ventrolateral parts of the striatum at all three examined levels^[6].
SCH 58261 diminishes the parkinsonian-like muscle rigidity and potentiates the effect of L-DOPA in rat model^[7].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	4‒6 weeks old athymic nude mice (NCI) with PC9 cells xenograft^[5]
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; daily; for 20 days
Result:	Decreased tumor growth.

分子量

345.36

Formula

C₁₈H₁₅N₇O

CAS 号

160098-96-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 34 mg/mL (98.45 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8955 mL	14.4776 mL	28.9553 mL
5 mM	0.5791 mL	2.8955 mL	5.7911 mL
10 mM	0.2896 mL	1.4478 mL	2.8955 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zocchi C, et al. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. Br J Pharmacol. 1996 Apr;117(7):1381-6.

[2]. Varani K, et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117(8):1693-701.

[3]. Xi J, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009 Nov;47(5):684-90.

[4]. Kuzumaki N, et al. Multiple analyses of G-protein coupled receptor (GPCR) expression in the development of gefitinib-resistance in transforming non-small-cell lung cancer. PLoS One. 2012;7(10):e44368.

[5]. Mediavilla-Varela M, et al. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Cancer Biol Ther. 2013 Sep;14(9):860-8.

[6]. Wardas J, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Brain Res. 2003 Jul 11;977(2):270-7.

[7]. Wardas J, et al. SCH 58261, an A(2A) adenosine receptor antagonist, counteracts parkinsonian-like muscle rigidity in rats. Synapse. 2001 Aug;41(2):160-71.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务