JAK2/FLT3-IN-1 TFA

发表于2024年5月14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。

JAK2/FLT3-IN-1 TFA 纯度: 98.94%

JAK2/FLT3-IN-1 (TFA) 是一种口服有效的双重 JAK2/FLT3 抑制剂，对 JAK2，FLT3，JAK1 和 JAK3 的 IC₅₀ 分别为 0.7 nM，4 nM，26 nM 和 39 nM。JAK2/FLT3-IN-1 (TFA) 具有抗癌活性。

JAK2/FLT3-IN-1 TFA Chemical Structure

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5 mg	￥7500	In-stock
10 mg	￥12500	In-stock
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JAK2/FLT3-IN-1 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity^[1].

IC₅₀ & Target

JAK1

26 nM (IC₅₀)

JAK2

0.7 nM (IC₅₀)

JAK3

39 nM (IC₅₀)

FLT3

4 nM (IC₅₀)

体外研究
(In Vitro)

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner^[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells^[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	MV4-11 and SET-2 cells
Concentration:	0.008, 0.04, 0.2, 1 μM
Incubation Time:	For 2 hours
Result:	Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis^[1]

Cell Line:	MV4-11 cells
Concentration:	5, 10, 50, 100 nM
Incubation Time:	For 2 hours
Result:	Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis^[1]

Cell Line:	MV4-11 cells
Concentration:	5, 10, 50, 100 nM
Incubation Time:	For 2 hours
Result:	Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.

体内研究
(In Vivo)

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects^[1].

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

Animal Model:	NOD/SCID mouse models^[1]
Dosage:	30 and 60 mg/kg
Administration:	Oral administration; daily; for 14 days
Result:	Exhibited significant antitumor effects. The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

分子量

581.61

Formula

C₂₇H₃₅F₄N₇O₃

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)

参考文献

[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.

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W146 TFA

发表于2024年5月10日由上海金畔生物科技有限公司

W146 TFA

W146 TFA 是 1-磷酸-鞘氨醇受体亚型 1 (S1PR1) 的选择性拮抗剂， EC₅₀ 值为 398 nM。

W146 TFA Chemical Structure

CAS No. : 909725-62-8

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生物活性

W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC₅₀ value of 398 nM.

IC₅₀ & Target

EC50: 398 nM (S1PR1)^[1].

体外研究
(In Vitro)

W146 is a S1PR1 antagonist with a K_i of ~70-80 nM^[1].
W146 pretreatment significantly increases activated cleaved caspase-3 levels. The reduced EPCs apoptosis which induced by S1P is completely abolished after treatment with W146^[2].

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

Apoptosis Analysis^[2]

Cell Line:	Endothelial progenitor cells (EPCs).
Concentration:	10 μM.
Incubation Time:	30 min before the addition of S1P.
Result:	Increases activated cleaved caspase-3 levels.

体内研究
(In Vivo)

W146 (5 mg/kg, ip, prior to AMD3100 administration) pre-treatment shows approximately 8-fold increase of KSL-HSPC mobilization, measured by the CFU-G/M colony forming assays, compared to that in mice treated with AMD3100 alone^[3]
The W146-mediated augmentation of KSL-HSPC mobilization is specific, because pretreatment of mice with W140 is unable to produce any effect on AMD3100-stimulated KSL-HSPC mobilization. Injections of W146, W140, JTE013, or Cay10444 do not alter the basal WBC count in mice^[3].

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

Animal Model:	Mice (4-6-week-old)^[3] .
Dosage:	5 mg/kg.
Administration:	IP, 1 hour prior to AMD3100 (ADM) administration.
Result:	Significantly increased in KSL-HSPC mobilization compared to that in mice pretreated with dextran followed by AMD3100 administration.

分子量

456.39

Formula

C₁₈H₂₈F₃N₂O₆P

CAS 号

909725-62-8

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]. M Germana Sanna, et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2006 Aug;2(8):434-41. Epub 2006 Jul 9.

[2]. Jingjing Liu, et al. 3-amino-4-(3-hexylphenylamino)-4-oxobutyl phosphonic acid (W146), a Selective Antagonist of Sphingosine-1-phospahte Receptor Subtype 1, Enhances AMD3100-stimulated Mobilization of Hematopoietic Stem Progenitor Cells in Animals. J Biochem Pharmacol Res. 2013 Dec; 1(4): 197–203.

[3]. Hang Wang, et al. Sphingosine-1-phosphate promotes the proliferation and attenuates apoptosis of Endothelial progenitor cells via S1PR1/S1PR3/PI3K/Akt pathway. Cell Biol Int. 2018 May 23.

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TLR7/8 agonist 4 TFA

发表于2024年5月5日由上海金畔生物科技有限公司

TLR7/8 agonist 4 TFA

TLR7/8 agonist 4 TFA (compound 41) 是一种有效的 TLR7/8 激动剂。TLR7/8 agonist 4 具有抗癌活性。

TLR7/8 agonist 4 TFA Chemical Structure

CAS No. : 2388520-34-9

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生物活性

TLR7/8 agonist 4 TFA (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity^[1].

IC₅₀ & Target^[1]

TLR7

TLR8

分子量

438.45

Formula

C₂₀H₂₅F₃N₆O₂

CAS 号

2388520-34-9

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]. Shelley Erin ACKERMAN, et al. Macromolecule-supported tlr agonists. WO2020190762A1.

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dTAGV-1 TFA

发表于2024年5月3日由上海金畔生物科技有限公司

dTAGV-1 TFA

dTAGV-1 TFA 是一种有效和选择性的突变 FKBP12^F36V 融合蛋白降解剂。dTAGV-1 TFA 可以在体内诱导 FKBP12^F36V-Nluc 降解。

dTAGV-1 TFA Chemical Structure

CAS No. : 2624313-15-9

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生物活性

dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12^F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12^F36V-Nluc in vivo^[1].

IC₅₀ & Target^[1]

VHL

体外研究
(In Vitro)

dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12^F36V-Nluc with no effects on FKBP12^WT-Nluc in 293FT cells^[1].
dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12^F36V and CDK9^[1].
dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRAS^G12V and pERK1/2 degradation^[1].
dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma^[1].

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

体内研究
(In Vivo)

dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12^F36V-Nluc in mice^[1].
dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T_1/2=3.64 and 4.4 h), C_max (595 and 2123 ng/mL) and great exposure (AUC_inf =3136 and 18517 h•ng/mL) in mice^[1].
dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T_1/2=3.02 h), C_max (7780 ng/mL) and great exposure (AUC_inf =3329 h•ng/mL) in mice^[1].

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

Animal Model:	8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12^F36V cells^[1]
Dosage:	35 mg/kg
Administration:	I.p. once daily for 4 days
Result:	Observed striking loss of bioluminescent signal 4 h after the first and three administrations. Degradation evident 28 h after the final administration.

分子量

1361.56

Formula

C₇₀H₉₁F₃N₆O₁₆S

CAS 号

2624313-15-9

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]. Nabet B, et, al. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat Commun. 2020 Sep 18;11(1):4687.

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GRGDSP TFA

发表于2024年5月1日由上海金畔生物科技有限公司

GRGDSP TFA 纯度: ≥98.0%

GRGDSP (TFA) 是一种整联蛋白 (integrin) 抑制剂。

GRGDSP TFA Chemical Structure

规格	价格	是否有货
1 mg	￥880	In-stock
5 mg	￥1650	In-stock
10 mg	￥2850	In-stock
50 mg		询价
100 mg		询价

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GRGDSP TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Peptidomimetic Library
Peptide Library

生物活性

GRGDSP (TFA) is an integrin inhibitor.

IC₅₀ & Target

Integrin^[1].

体外研究
(In Vitro)

It is demonstrated that transarterial infusion of GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro integrin-inhibitor which includes RGD-peptide). As a synthetic linear RGD peptide, GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis^[1]. GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) is used as a soluble integrin-blocking RGD-based peptide. GRGDSP is used widely together with other RGD peptides in integrin research. GRGDSP can be used to modify the surface of cardiovascular implants such as vascular grafts to promote endothelialization^[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

701.61

Formula

C₂₄H₃₈F₃N₉O₁₂

Sequence

Gly-Arg-Gly-Asp-Ser-Pro

Sequence Shortening

GRGDSP

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

H₂O : 125 mg/mL (178.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4253 mL	7.1265 mL	14.2529 mL
5 mM	0.2851 mL	1.4253 mL	2.8506 mL
10 mM	0.1425 mL	0.7126 mL	1.4253 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]. Qian J, et al. Transarterial administration of integrin inhibitor loaded nanoparticles combined with transarterial chemoembolization for treating hepatocellular carcinoma in a rat model. World J Gastroenterol. 2016 Jun 7;22(21):5042-9.

[2]. Patel S, et al. Regulation of endothelial cell function by GRGDSP peptide grafted on interpenetrating polymers. J Biomed Mater Res A. 2007 Nov;83(2):423-33.

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ATI-2341 TFA

发表于2024年4月30日由上海金畔生物科技有限公司

ATI-2341 TFA 纯度: 98.11%

ATI-2341 是一种有效的 C-X-C 趋化因子受体 4 型 (CXCR4) 功能选择性变构激动剂，其作为偏向配体起作用，有利于 Gα1激活而不是 Gα13。ATI-2341 激活抑制性异源三聚体 G 蛋白 (Gi) 以促进 cAMP 产生的抑制并诱导钙动员。ATI-2341 是一种有效骨髓多形核中性粒细胞 (PMNs) 和造血干细胞和祖细胞 (HSPCs) 动员剂。

ATI-2341 TFA Chemical Structure

规格	价格	是否有货
1 mg	￥1400	In-stock
5 mg	￥3900	In-stock
10 mg	￥6100	In-stock
50 mg		询价
100 mg		询价

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ATI-2341 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Peptide Library

生物活性

ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs)^[1]^[2].

体外研究
(In Vitro)

CXCR4^[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

2370.84

Formula

C₁₀₆H₁₇₉F₃N₂₆O₂₇S₂

Sequence Shortening

1-Oxohexadecyl-MGYQKKLRSMTDKYRL

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL (42.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.4218 mL	2.1090 mL	4.2179 mL
5 mM	0.0844 mL	0.4218 mL	0.8436 mL
10 mM	0.0422 mL	0.2109 mL	0.4218 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：

——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 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (1.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.05 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (1.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.05 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]. Quoyer J, et al. Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein. Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):E5088-97.

[2]. Tchernychev B, et al. Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells. Proc Natl Acad Sci U S A. 2010 Dec 21;107(51):22255-9.

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DTP3 TFA

发表于2024年4月14日由上海金畔生物科技有限公司

DTP3 TFA 纯度: 98.75%

DTP3 TFA 是一种有效且选择性的 GADD45β/MKK7 抑制剂。DTP3 TFA 靶向 NF-κB 途径下游，具有抗癌活性。

DTP3 TFA Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2251	In-stock
5 mg	￥1600	In-stock
10 mg	￥2800	In-stock
25 mg	￥4000	In-stock
50 mg	￥5500	In-stock
100 mg	￥8000	In-stock
200 mg		询价
500 mg		询价

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DTP3 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
NF-κB Signaling Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Reprogramming Compound Library
Oxygen Sensing Compound Library
Anti-Blood Cancer Compound Library
Anti-Parkinson’s Disease Compound Library
Anti-Obesity Compound Library
Transcription Factor Targeted Library
Peptide Library

生物活性

DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway^[1].

IC₅₀ & Target

GADD45β/MKK7^[1]

体外研究
(In Vitro)

DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours^[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.

Western Blot Analysis^[2]

Cell Line:	Multiple myeloma (MM) cell lines
Concentration:	10 μM
Incubation Time:	1, 3, 5, 14, 21 days
Result:	Caused the appearance of phosphorylated JNK, as early as 24 hours.

体内研究
(In Vivo)

DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice^[2].
DTP3 TFA (intravenous injection; 10 mg/kg/day) has t_1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and V_d of 2.80 L/kg^[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:	6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)^[2]
Dosage:	14.5 mg/kg
Administration:	S.c.; daily; 28 days
Result:	Had shown a dramatic shrinkage of the tumors.

Animal Model:	CD1 male mice of 25-30 g^[2]
Dosage:	10 mg/kg (Pharmacokinetic Study)
Administration:	Intravenous injection
Result:	Had t_1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and V_d of 2.80 L/kg.

分子量

639.62

Formula

C₂₈H₃₆F₃N₇O₇

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

H₂O : 100 mg/mL (156.34 mM; Need ultrasonic)

DMSO : 50 mg/mL (78.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5634 mL	7.8171 mL	15.6343 mL
5 mM	0.3127 mL	1.5634 mL	3.1269 mL
10 mM	0.1563 mL	0.7817 mL	1.5634 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 and 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：

1.

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

Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.91 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]. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.

[2]. Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508.

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

DAMGO (TFA)

发表于2024年4月12日由上海金畔生物科技有限公司

DAMGO (TFA) 纯度: 99.76%

DAMGO TFA 是一种选择性的 μ-阿片受体 (μ-OPR) 激动剂，K_d 值为 3.46 nM。

DAMGO (TFA) Chemical Structure

CAS No. : 950492-85-0

规格	价格	是否有货
10 mM * 1 mL in Water	￥1367	In-stock
1 mg	￥600	In-stock
5 mg	￥990	In-stock
10 mg	￥1700	In-stock
25 mg	￥3700	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

DAMGO (TFA) 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Neuronal Signaling Compound Library
Anti-Cancer Compound Library
Neurotransmitter Receptor Compound Library
Peptide Library

生物活性

DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR^[1].

分子量

627.61

Formula

C₂₈H₃₆F₃N₅O₈

CAS 号

950492-85-0

Sequence

Tyr-{d-Ala}-Gly-{Me-Phe}-Gly-ol

Sequence Shortening

Y-{d-Ala}-G-{Me-Phe}-G-ol

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

H₂O : 125 mg/mL (199.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5933 mL	7.9667 mL	15.9335 mL
5 mM	0.3187 mL	1.5933 mL	3.1867 mL
10 mM	0.1593 mL	0.7967 mL	1.5933 mL

参考文献

[1]. FEBS Lett. 1995 Jan 2;357(1):93-7. Onogi T, et al. DAMGO, a mu-opioid receptor selective agonist, distinguishes between mu- and delta-opioid receptors around their first extracellular loops.

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

SETD2-IN-1 TFA

发表于2024年4月11日由上海金畔生物科技有限公司

SETD2-IN-1 TFA 纯度: 99.42%

SETD2-IN-1 TFA 是一种有效、选择性和具有口服活性的人类组蛋白甲基转移酶 SETD2 抑制剂。SETD2-IN-1 TFA 具有抗增殖作用。

SETD2-IN-1 TFA Chemical Structure

CAS No. : 2411759-92-5

规格	价格	是否有货
5 mg	￥5000	In-stock
10 mg	￥8500	In-stock
25 mg	￥18000	In-stock
50 mg	￥30000	In-stock
100 mg	￥46000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

SETD2-IN-1 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

SETD2-IN-1 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. SETD2-IN-1 TFA has anti-proliferative effects^[1].

IC₅₀ & Target

SETD2^[1]

分子量

514.51

Formula

C₂₄H₃₀F₄N₄O₄

CAS 号

2411759-92-5

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 : 200 mg/mL (388.72 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9436 mL	9.7180 mL	19.4360 mL
5 mM	0.3887 mL	1.9436 mL	3.8872 mL
10 mM	0.1944 mL	0.9718 mL	1.9436 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: ≥ 5 mg/mL (9.72 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.72 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (9.72 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.72 mM，饱和度未知) 的澄清溶液。

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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 5 mg/mL (9.72 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.72 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 50.0 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]. John Lampe, et al. Substituted indoles and methods of use thereof. WO2020037079A1.

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

Pomalidomide-PEG3-C2-NH2 TFA(Synonyms: Cereblon Ligand-Linker Conjugates 5 TFA; E3 ligase Ligand-Linker Conjugates 30 TFA)

发表于2024年4月9日由上海金畔生物科技有限公司

Pomalidomide-PEG3-C2-NH2 TFA (Synonyms: Cereblon Ligand-Linker Conjugates 5 TFA; E3 ligase Ligand-Linker Conjugates 30 TFA) 纯度: 99.0%

Pomalidomide-PEG3-C2-NH2 TFA 是一种合成的 E3 连接酶配体-linker 偶联物，包含基于 Pomalidomide 的 cereblon 配体和 3 个单元 PEG 的 linker。

Pomalidomide-PEG3-C2-NH2 TFA Chemical Structure

CAS No. : 2414913-97-4

规格	价格	是否有货
100 mg	￥3500	In-stock
500 mg	￥13500	In-stock
1 g	￥25000	询价
2 g	￥35000	询价
5 g		询价
10 g		询价

* Please select Quantity before adding items.

生物活性

Pomalidomide-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

IC₅₀ & Target^[1]

Cereblon

分子量

562.49

Formula

C₂₃H₂₉F₃N₄O₉

CAS 号

2414913-97-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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 : 100 mg/mL (177.78 mM; Need ultrasonic)

Ethanol : 100 mg/mL (177.78 mM; Need ultrasonic)

H₂O : 16.67 mg/mL (29.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7778 mL	8.8890 mL	17.7781 mL
5 mM	0.3556 mL	1.7778 mL	3.5556 mL
10 mM	0.1778 mL	0.8889 mL	1.7778 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： PBS

Solubility: 50 mg/mL (88.89 mM); Clear 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 (4.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.44 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 (4.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.44 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 (4.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.44 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]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression. J Med Chem. 2019 Jan 24;62(2):448-466.

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

Thalidomide-O-amido-C3-NH2 TFA(Synonyms: Cereblon Ligand-Linker Conjugates 16 TFA; E3 Ligase Ligand-Linker Conjugates 52 TFA)

发表于2024年4月8日由上海金畔生物科技有限公司

Thalidomide-O-amido-C3-NH2 TFA (Synonyms: Cereblon Ligand-Linker Conjugates 16 TFA; E3 Ligase Ligand-Linker Conjugates 52 TFA) 纯度: 98.18%

Thalidomide-O-amido-C3-NH2 TFA 是一种合成的 E3 连接酶配体-linker 偶联物，包含基于 Thalidomide 的 cereblon 配体和 1 个 linker。

Thalidomide-O-amido-C3-NH2 TFA Chemical Structure

CAS No. : 2022182-58-5

规格	价格	是否有货
5 mg	￥600	In-stock
10 mg	￥1000	In-stock
50 mg	￥3000	In-stock
100 mg	￥5000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

IC₅₀ & Target

Cereblon

分子量

502.40

Formula

C₂₀H₂₁F₃N₄O₈

CAS 号

2022182-58-5

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 : 125 mg/mL (248.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9904 mL	9.9522 mL	19.9045 mL
5 mM	0.3981 mL	1.9904 mL	3.9809 mL
10 mM	0.1990 mL	0.9952 mL	1.9904 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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.14 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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.14 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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.14 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]. Lohbeck J, et al. Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5260-5262.

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

Epitalon TFA(Synonyms: Epithalon TFA; Epithalamin TFA)

发表于2024年4月6日由上海金畔生物科技有限公司

Epitalon TFA (Synonyms: Epithalon TFA; Epithalamin TFA) 纯度: 99.23%

Epitalon TFA 是一种抗衰老剂和端粒酶激活剂。Epitalon TFA 对小鼠自发性肿瘤的发展具有抑制作用，具有 geroprotective 作用，通过鼻内给药可增加神经元活性。Epitalon TFA 可用于癌症，衰老和色素性视网膜炎。

Epitalon TFA Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2160	In-stock
1 mg	￥650	In-stock
5 mg	￥1950	In-stock
10 mg	￥3500	In-stock
25 mg	￥7500	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

Epitalon TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Rare Diseases Drug Library
Peptide Library

生物活性

Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa^[1].

体外研究
(In Vitro)

Addition of Epithalon peptide in telomerase-negative human fetal fibroblast culture induced expression of the catalytical subunit, enzymatic activity of telomerase, and telomere elongation, which can be due to reactivation of telomerase gene in somatic cells and indicates the possibility of prolonging life span of a cell population and of the whole organism^[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)

Epitalon TFA increases the lifespan of mice and fruit flies and restores the circadian rhythms of melatonin and cortisol production in old rhesus monkeys. At the same time, Epitalon prolongs the functional integrity of the eye retina in Campbell rats with hereditary Retinitis Pigmentosa and improves the visual functions in patients with pigmental retinal degeneration^[1].
Epitalon TFA (subcutaneous injection; 1.0 µg/mouse (30-40 µg/kg); 5 consecutive days every month; 3-12 months) does not influence food consumption, body weight or mean life span of mice. However, Epitalon slows down the age-related switching-off of estrous function and decreased the frequency of chromosome aberrations in bone marrow cells (by 17.1%). Epitalon increased by 13.3% the life span of the last 10% of the survivors in comparison with the control group in Swiss-derived SHR mice^[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.

Animal Model:	Swiss-derived SHR mice^[4]
Dosage:	1.0 µg/mouse (∼30-40 µg/kg)
Administration:	Subcutaneous injection; 1.0 µg/mouse (∼30-40 µg/kg) ; 5 consecutive days every month; 3-12 months
Result:	Significantly decreased the age-associated increase in chromosome aberrations after long-term treatment.

分子量

504.37

Formula

C₁₆H₂₃F₃N₄O₁₁

Sequence Shortening

AEDG

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Stored under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

DMSO : 250 mg/mL (495.67 mM; Need ultrasonic)

H₂O : 100 mg/mL (198.27 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9827 mL	9.9134 mL	19.8267 mL
5 mM	0.3965 mL	1.9827 mL	3.9653 mL
10 mM	0.1983 mL	0.9913 mL	1.9827 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 (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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 (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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 (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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]. Khavinson VKh. et al. Peptides and Ageing. Neuro Endocrinol Lett. 2002;23 Suppl 3:11-144.

[2]. Vanhee C, et al. Identification of the small research tetra peptide Epitalon, assumed to be a potential treatment for cancer, old age and Retinitis Pigmentosa in two illegal pharmaceutical preparations. Drug Test Anal. 2015 Mar;7(3):259-64.

[3]. Khavinson VKh, et al. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003 Jun;135(6):590-2.

[4]. Vladimir N Anisimov, et al.Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology. 2003;4(4):193-202

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WL47 TFA

发表于2024年3月20日由上海金畔生物科技有限公司

WL47 TFA 纯度: 99.70%

WL47 TFA 是一种高亲和力的 cavolin-1 (CAV1) ligand (K_d=23 nM)，是一种有效的 CAV1 寡聚体破坏剂。WL47 TFA 对 CAV1 的选择性高于 BSA、酪蛋白和 HEWL。WL47 TFA 比原始 T20 (HY-P0052) 亲本序列长度小 80%，可用于 caveolin-1 功能的研究。

WL47 TFA Chemical Structure

规格	价格	是否有货
1 mg	￥1200	In-stock
5 mg	￥3500	询价
10 mg		询价
50 mg		询价

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WL47 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

WL47 TFA, a high-affinity cavolin-1 (CAV1) ligand (K_d=23 nM), is a potent disrupter of CAV1 oligomers. WL47 TFA shows selectivity for CAV1 over BSA, casein and HEWL. WL47 TFA is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function^[1].

IC₅₀ & Target

Kd: 23 nM (cavolin-1)^[1]

体外研究
(In Vitro)

Caveolin-1 (CAV) is a monotonic membrane protein, 22 kDa, it penetrates only one leaflet of the lipid bilayer, and both the N- and C-termini remain on the cytoplasmic side. Multiple copies of CAV oligomerize can form high molecular weight complexes that bend the membrane inward to form invaginations, termed “caveolae,” of 50-100 nm in diameter.
T20 is a 36 amino acid peptide derived from gp41 and blocks HIV viral fusion with CD4⁺ T-cells. WL47 is 80% smaller in length and has 7500-fold greater affinity than the original T20 parent sequence.
In vitro, Demonstrating WL47 activity with CAV oligomers and a method for measuring the degree of oligomerization. A variant of CAV (CAV(FLV)) that spontaneously oligomerizes to form CAV nanoparticles with diameters is used to examine deoligomerization by WL47. WL47 effectively disrupts these nanoparticles, but it does not disrupt oligomerization in the presence of a reducing agent, this demonstating that WL47 function requires dimerization by disulfide bond

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

1958.32

Formula

C₈₂H₁₃₁N₂₄F₃O₂₀S₄

Sequence

Lys-Leu-Arg-Met-Trp-Ser-Cys-Cys-Ser-Trp-Met-Arg-Leu-Lys

Sequence Shortening

KLRMWSCCSWMRLK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

DMSO : 50 mg/mL (25.53 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5106 mL	2.5532 mL	5.1064 mL
5 mM	0.1021 mL	0.5106 mL	1.0213 mL
10 mM	0.0511 mL	0.2553 mL	0.5106 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 (1.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.28 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 (1.28 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (1.28 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 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 (1.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.28 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]. Amanda J H Gilliam,et al. Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization. J Med Chem. 2016 Apr 28;59(8):4019-25.

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Fz7-21 TFA(Synonyms: Ac-LPSDDLEFWCHVMY-NH2 TFA)

发表于2024年3月16日由上海金畔生物科技有限公司

Fz7-21 TFA (Synonyms: Ac-LPSDDLEFWCHVMY-NH2 TFA) 纯度: 99.87%

Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA 是 Frizzled 7 (FZD 7) 受体的肽拮抗剂，选择性地与 FZD7 CRD 亚类结合。在人和小鼠 FZD7 CRD 中的 EC₅₀ 值分别为 58 和 34 nM。Fz7-21 TFA 对外源性 WNT3A (IC₅₀=100 nM) 刺激和转染 WNT3A 或 WNT1 的 HEK293 细胞 Wnt/β-catenin 信号传导有损伤。Fz7-21 TFA 还阻断了 WNT3A 介导的 β-catenin 在小鼠 L 细胞中的稳定作用 (IC₅₀=50 nM)。

Fz7-21 TFA Chemical Structure

规格	价格	是否有货
5 mg	￥2900	In-stock
10 mg	￥4600	In-stock
50 mg	￥13500	In-stock
100 mg		询价
200 mg		询价

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Fz7-21 TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Stem Cell Signaling Compound Library
Wnt/Hedgehog/Notch Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Cytoskeleton Compound Library
Neuroprotective Compound Library
Anti-Breast Cancer Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library
Peptide Library

生物活性

Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC₅₀ values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC₅₀=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC₅₀=50 nM)^[1].

IC₅₀ & Target

EC50: 58 nM (human FZD7 CRD), 34 nM (mouse FZD7 CRD)^[1]

分子量

1910.07

Formula

C₈₅H₁₁₅N₁₈F₃O₂₅S₂

Sequence Shortening

Ac-LPSDDLEFWCHVMY-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (17.45 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5235 mL	2.6177 mL	5.2354 mL
5 mM	0.1047 mL	0.5235 mL	1.0471 mL
10 mM	0.0524 mL	0.2618 mL	0.5235 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: 2.5 mg/mL (1.31 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (1.31 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 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (1.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.31 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]. Nile AH, et al. Publisher Correction: A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells. Nat Chem Biol. 2018 Sep;14(9):902.

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Endothelin-2 (49-69), human TFA(Synonyms: Endothelin-2 (49-69) (human, canine) TFA; Human endothelin-2 TFA)

发表于2024年3月16日由上海金畔生物科技有限公司

Endothelin-2 (49-69), human TFA (Synonyms: Endothelin-2 (49-69) (human, canine) TFA; Human endothelin-2 TFA) 纯度: 99.82%

Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) 是由 21 个氨基酸组成的血管活性肽，可与 G 蛋白连接的跨膜受体，ET-RA 和 ET-RB 结合。

Endothelin-2 (49-69), human TFA Chemical Structure

规格	价格	是否有货	数量
500 μg	￥3120	In-stock

* Please select Quantity before adding items.

Endothelin-2 (49-69), human TFA 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Peptide Library

生物活性

Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

体外研究
(In Vitro)

At nanomolar concentrations, Endothelin-2 exhibits a strong and long-lasting vasoconstrictor activity characteristic of endothelin (EC₅₀=0.52 nM)^[1].
Endothelin-2 is a chemoattractant for macrophages and THP-1 monocytic cells, but not for freshly isolated monocytes. The chemotactic response to Endothelin-2 shows a typical bell-shaped response curve. Experiments with endothelin receptor antagonists shows that migration to Endothelin-2 is mediated via the ET-RB receptor. Endothelin-2 expression by tumors may modulate the behavior of macrophages such that activated cells accumulate in areas of hypoxia^[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.

体内研究
(In Vivo)

Two distinct phases of pressor effects are typically seen in response to Endothelin-2: the early phase immediately follows the depressor response and dominates during the next 3-10 min, whereas the late pressor effect develops 10-20 min after the injection and lasts >1 hr^[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

2660.94

Formula

C₁₁₇H₁₆₁N₂₆F₃O₃₄S₄

Sequence

Cys-Ser-Cys-Ser-Ser-Trp-Leu-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp (Disulfide bridge: Cys1-Cys15, Cys3-Cys11)

Sequence Shortening

CSCSSWLDKECVYFCHLDIIW (Disulfide bridge: Cys1-Cys15, Cys3-Cys11)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

H₂O : 6.67 mg/mL (2.51 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.3758 mL	1.8790 mL	3.7581 mL
5 mM	—	—	—
10 mM	—	—	—

参考文献

[1]. Grimshaw MJ, et al. Endothelin-2 is a macrophage chemoattractant: implications for macrophage distribution in tumors. Eur J Immunol. 2002 Sep;32(9):2393-400.

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Cyclic MKEY TFA

发表于2024年3月15日由上海金畔生物科技有限公司

Cyclic MKEY TFA

Cyclic MKEY TFA 是 CXCL4-CCL5 异二聚体形成的合成环肽抑制剂，其通过介导炎症来防止动脉粥样硬化和主动脉瘤形成。Cyclic MKEY TFA 还可以预防小鼠中风引起的脑损伤。

Cyclic MKEY TFA Chemical Structure

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生物活性	Cyclic MKEY TFA is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY TFA also protects against stroke-induced brain injury in mice^[1]^[2].
IC₅₀ & Target	CXCL4-CCL5^[1]
分子量	2646.91
Formula	C₁₁₅H₁₇₅N₂₈F₃O₃₆S₂
Sequence Shortening	CKEYFYTSSKSSNLAVVFVTRC
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]. Fan Y,et al. MKEY, a Peptide Inhibitor of CXCL4-CCL5 Heterodimer Formation, Protects Against Stroke in Mice. J Am Heart Assoc. 2016 Sep 15;5(9). pii: e003615. [2]. Iida Y, et al. Peptide inhibitor of CXCL4-CCL5 heterodimer formation, MKEY, inhibits experimental aortic aneurysm initiation and progression. Arterioscler Thromb Vasc Biol. 2013 Apr;33(4):718-26.

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Ac-IEVDIDVEH TFA

发表于2024年3月14日由上海金畔生物科技有限公司

Ac-IEVDIDVEH TFA

Ac-IEVDIDVEH TFA 是一个短肽序列，末端是 Ac。

Ac-IEVDIDVEH TFA Chemical Structure

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

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生物活性	Ac-IEVDIDVEH TFA is a short peptide sequence with Ac at the end.
分子量	1224.19
Formula	C₅₀H₇₆F₃N₁₁O₂₁
Sequence	Ac-Ile-Glu-Val-Asp-Ile-Asp-Val-Glu-His
Sequence Shortening	Ac-IEVDIDVEH
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.

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Ac-IEVDIDVE TFA

发表于2024年3月14日由上海金畔生物科技有限公司

Ac-IEVDIDVE TFA

Ac-IEVDIDVE TFA 是一个短肽序列，末端是 Ac。

Ac-IEVDIDVE TFA Chemical Structure

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生物活性	Ac-IEVDIDVE TFA is a short peptide sequence with Ac at the end.
分子量	1087.06
Formula	C₄₄H₆₉F₃N₈O₂₀
Sequence	Ac-Ile-Glu-Val-Asp-Ile-Asp-Val-Glu
Sequence Shortening	Ac-IEVDIDVE
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.

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Ac-IEVDIDV TFA

发表于2024年3月14日由上海金畔生物科技有限公司

Ac-IEVDIDV TFA

Ac-IEVDIDV TFA 是一个短肽序列，末端是 Ac。

Ac-IEVDIDV TFA Chemical Structure

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100 mg		询价
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500 mg		询价

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生物活性	Ac-IEVDIDV TFA is a short peptide sequence with Ac at the end.
分子量	957.94
Formula	C₃₉H₆₂F₃N₇O₁₇
Sequence	Ac-Ile-Glu-Val-Asp-Ile-Asp-Val
Sequence Shortening	Ac-IEVDIDV
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.

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Ac-IEVDID TFA

发表于2024年3月13日由上海金畔生物科技有限公司

Ac-IEVDID TFA

Ac-IEVDID TFA 是一个短肽序列，末端是 Ac。

Ac-IEVDID TFA Chemical Structure

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100 mg		询价
250 mg		询价
500 mg		询价

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生物活性	Ac-IEVDID TFA is a short peptide sequence with Ac at the end.
分子量	858.81
Formula	C₃₄H₅₃F₃N₆O₁₆
Sequence	Ac-Ile-Glu-Val-Asp-Ile-Asp
Sequence Shortening	Ac-IEVDID
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.

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