STING agonist-7

发表于2023年11月5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。

STING agonist-7

STING agonist-7 是一种非核苷酸 STING 激动剂，选择性结合小鼠 STING 而不是人类 STING。STING agonist-7 穿透细胞膜较差。

STING agonist-7 Chemical Structure

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生物活性	STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly^[1].
体外研究 (In Vitro)	STING agonist-7 (compound 11) is active in biochemical assays but inactive in cellular reporter assays^[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	336.30
Formula	C₁₇H₁₂N₄O₄
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]. Emily C Cherney, et al. Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization. J Med Chem. 2022 Feb 24;65(4):3518-3538.

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TLX agonist 1

发表于2023年10月27日由上海金畔生物科技有限公司

TLX agonist 1 纯度: 99.82%

TLX agonist 1 (ccrp2) 是一种孤核受体 tailless (TLX, NR2E1) 调节剂 (EC₅₀=1 μM; K_d= 650 nM)。TLX agonist 1 增强 TLX 转录抑制活性。

TLX agonist 1 Chemical Structure

CAS No. : 958323-31-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥1500	In-stock
10 mg	￥2300	In-stock
25 mg	￥4600	In-stock
50 mg	￥7500	In-stock
100 mg	￥12000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

TLX agonist 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC₅₀=1μM; K_d= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity^[1].

分子量

374.48

Formula

C₂₃H₂₆N₄O

CAS 号

958323-31-4

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 : 62.5 mg/mL (166.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6704 mL	13.3518 mL	26.7037 mL
5 mM	0.5341 mL	2.6704 mL	5.3407 mL
10 mM	0.2670 mL	1.3352 mL	2.6704 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：

——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: ≥ 2.08 mg/mL (5.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.55 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 (5.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.55 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 (5.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.55 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 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Benod C, et al. The human orphan nuclear receptor tailless (TLX, NR2E1) is druggable. PLoS One. 2014 Jun 17;9(6):e99440.

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diABZI STING agonist-1 trihydrochloride

发表于2023年10月11日由上海金畔生物科技有限公司

diABZI STING agonist-1 trihydrochloride 纯度: 99.92%

diABZI STING agonist-1 (trihydrochloride) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC₅₀ 值分分别为 130 nM 和 186 nM。

diABZI STING agonist-1 trihydrochloride Chemical Structure

CAS No. : 2138299-34-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥6300	In-stock
5 mg	￥3500	In-stock
10 mg	￥5900	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

diABZI STING agonist-1 trihydrochloride 相关产品

•相关化合物库:

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Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library

生物活性

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

IC₅₀ & Target

STING^[1].

体外研究
(In Vitro)

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested^[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)

diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo^[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC₅₀) for mouse STING (200 ng/ml)^[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43^[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:	Wild and Sting^−/− C57Blk6 mice^[1]
Dosage:	2.5 mg/kg
Administration:	Subcutaneous injection; 2.5 mg/kg
Result:	Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting^−/− mice.

Animal Model:	Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:	3 mg/kg
Administration:	Intravenous injection; 3 mg/kg
Result:	Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC₅₀ for mouse STING (200 ng/ml).

Animal Model:	Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:	1.5 mg/kg
Administration:	Intravenous injection; 1.5 mg/kg; 43 days
Result:	Resulted in significant tumour growth inhibition and improved survival.

分子量

959.32

Formula

C₄₂H₅₄Cl₃N₁₃O₇

CAS 号

2138299-34-8

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:

H₂O : 100 mg/mL (104.24 mM; Need ultrasonic)

DMSO : 90 mg/mL (93.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0424 mL	5.2120 mL	10.4241 mL
5 mM	0.2085 mL	1.0424 mL	2.0848 mL
10 mM	0.1042 mL	0.5212 mL	1.0424 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。

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 (2.17 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.17 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 (2.17 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.17 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 (2.17 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.17 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]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.

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BMP signaling agonist sb4

发表于2023年9月14日由上海金畔生物科技有限公司

BMP signaling agonist sb4 纯度: 99.89%

BMP signaling agonist sb4 是一种有效的苯并恶唑骨形态发生蛋白 4 (BMP4) 信号激动剂，EC₅₀ 值为 74 nM，通过稳定细胞内 p-SMAD-1/5/9 激活 BMP 信号。BMP signaling agonist sb4 还能激活典型 BMP 信号通路中的 BMP4 靶基因 (DNA 结合抑制剂，Id1 和 Id3)。

BMP signaling agonist sb4 Chemical Structure

CAS No. : 100874-08-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥800	In-stock
10 mg	￥800	In-stock
50 mg	￥2100	In-stock
100 mg	￥3750	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BMP signaling agonist sb4 相关产品

•相关化合物库:

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Kinase Inhibitor Library
TGF-beta/Smad Compound Library
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Differentiation Inducing Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library

生物活性

BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC₅₀ value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling^[1].

IC₅₀ & Target

IC50: BMP4 signal^[1]

体外研究
(In Vitro)

BMP signaling agonist sb4 (0.05 μM-1 μM; 24 hours) induces phosphorylated SMAD-1/5/9 in a dose-dependent manner in PRECs cells under serum-starved conitions^[1].
BMP signaling agonist sb4 (1 μM; 0-60 mins) enhances the efficacy of signaling at each concentration of rhBMP4 tested. This effect is most pronounced at low concentrations of rhBMP4, whereby sb4 increases BRE-luc expression 2-fold at 0.4 ng/ml of rhBMP4^[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.

Western Blot Analysis^[1]

Cell Line:	Primary mouse kidney epithelial cells (PRECs)
Concentration:	0.05 μM-1 μM
Incubation Time:	24 hours
Result:	Incresed p-SMAD-1/5/9 abundance in PRECs.

Western Blot Analysis^[1]

Cell Line:	BRE-Luc cells
Concentration:	1 μM
Incubation Time:	0min, 5 mins, 15 mins, 30 mins, 45 mins, 60 mins
Result:	Acted to stabilize p-SMAD-1/5/9 to enhance the transcriptional response.

分子量

320.20

Formula

C₁₄H₁₀BrNOS

CAS 号

100874-08-6

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 (312.30 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1230 mL	15.6152 mL	31.2305 mL
5 mM	0.6246 mL	3.1230 mL	6.2461 mL
10 mM	0.3123 mL	1.5615 mL	3.1230 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: ≥ 6.25 mg/mL (19.52 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (19.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 62.5 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 (7.81 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.81 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 (7.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.81 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]. Bradford STJ, et al. High-throughput screens for agonists of bone morphogenetic protein (BMP) signaling identify potent benzoxazole compounds.J Biol Chem. 2019 Mar 1;294(9):3125-3136.

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STING agonist-3

发表于2023年9月1日由上海金畔生物科技有限公司

STING agonist-3 纯度: 99.96%

STING agonist-3 源于专利 WO2017175147A1 (实施例10)，是一种选择性和非核苷酸的小分子 STING 激动剂，pEC₅₀ 和 pIC₅₀ 分别为 7.5 和 9.5。STING agonist-3 具有持久的抗肿瘤作用，并且在改善癌症研究方面具有巨大潜力。

STING agonist-3 Chemical Structure

CAS No. : 2138299-29-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5780	In-stock
5 mg	￥4000	In-stock
10 mg	￥7000	In-stock
25 mg	￥11000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

STING agonist-3 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library

生物活性

STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC₅₀ and pIC₅₀ of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer^[1].

体外研究
(In Vitro)

STING agonist-3 exhibits a pEC₅₀ value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter^[1].
STING agonist-3 exhibits a pIC₅₀ value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING^[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

750.81

Formula

C₃₇H₄₂N₁₂O₆

CAS 号

2138299-29-1

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 : 41.67 mg/mL (55.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3319 mL	6.6595 mL	13.3189 mL
5 mM	0.2664 mL	1.3319 mL	2.6638 mL
10 mM	0.1332 mL	0.6659 mL	1.3319 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 (2.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.77 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 (2.77 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (2.77 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 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 (2.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.77 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]. Adam Kenneth, et al. Heterocyclic amides useful as protein modulators.patent WO2017175147A1

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1V209(Synonyms: TLR7 agonist T7)

发表于2023年8月30日由上海金畔生物科技有限公司

1V209 (Synonyms: TLR7 agonist T7) 纯度: 99.52%

1V209 (TLR7 agonist T7) 是 Toll-like receptor 7 (TLR7) 激动剂，具有抗肿瘤作用。1V209 可与各种多糖缀合，以改善其水溶性，增强功效并保持低毒性。

1V209 Chemical Structure

CAS No. : 1062444-54-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1383	In-stock
1 mg	￥580	In-stock
5 mg	￥1750	In-stock
10 mg	￥3000	In-stock
25 mg	￥6000	In-stock
50 mg	￥9000	In-stock
100 mg	￥13500	In-stock
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1V209 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library
Antioxidants Compound Library
Reprogramming Compound Library
Oxygen Sensing Compound Library
Pyroptosis Compound Library
Anti-Breast Cancer Compound Library

生物活性

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity^[1]^[2].

IC₅₀ & Target^[1]

TLR7

体外研究
(In Vitro)

1V209 (0.1-10 μM) treatment significantly stimulates TNFα production in RAW246.7 cells^[1].
1V209 (18 hours) treatment increases IL-6 production comparain bone marrow derived dendritic 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)

The intravenous (IV) administration of the formulation to mice bearing 4T1 breast cancer tumors results in nanoparticle accumulation in tumors, reduction in primary tumor growth, and inhibition of lung metastases, as compared to saline-treated animals. Mice administered 1V209 experience significantly increases plasma levels of proinflammatory cytokines IL-6, IP-10, and MCP-1 at 2 h following IV administration^[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

359.34

Formula

C₁₆H₁₇N₅O₅

CAS 号

1062444-54-5

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 : 83.33 mg/mL (231.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7829 mL	13.9144 mL	27.8288 mL
5 mM	0.5566 mL	2.7829 mL	5.5658 mL
10 mM	0.2783 mL	1.3914 mL	2.7829 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 (5.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.79 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 (5.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.79 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]. Battistella C, et al. Delivery of Immunotherapeutic Nanoparticles to Tumors via Enzyme-Directed Assembly. Adv Healthc Mater. 2019 Dec;8(23):e1901105.

[2]. Shinchi H, et al. Enhancement of the Immunostimulatory Activity of a TLR7 Ligand by Conjugation to Polysaccharides. Bioconjug Chem. 2015 Aug 19;26(8):1713-23.

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GPR35 agonist 1

发表于2023年8月29日由上海金畔生物科技有限公司

GPR35 agonist 1

GPR35 agonist 1 (compound 50) 是一种高效特异性的 GPR35/CXCR8 激动剂，EC₅₀ 值为 5.8 nM，具有很好的成药性。

GPR35 agonist 1 Chemical Structure

CAS No. : 2079880-92-3

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生物活性	GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC₅₀ of 5.8 nM, displays good druggability^[1].
IC₅₀ & Target	EC50: 5.8 nM (GPR35/CXCR8)^[1]
分子量	354.07
Formula	C₁₀H₄BrN₅O₅
CAS 号	2079880-92-3
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]. Wei L, et al. Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists. J Med Chem. 2017 Jan 12;60(1):362-372.

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RORγt agonist 1

发表于2023年8月23日由上海金畔生物科技有限公司

RORγt agonist 1

RORγt agonist 1 (compound 14) 是有效的，口服生物可利用的 RORγt 激动剂，EC₅₀ 为 20.8 nM。RORγt agonist 1 显示出高代谢稳定性，改善的水溶性和优异的小鼠 PK 特征。RORγt agonist 1 是用于癌症免疫疗法的 RORγt 激动剂的潜在候选物。

RORγt agonist 1 Chemical Structure

CAS No. : 2377378-89-5

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生物活性	RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC₅₀ of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy^[1].
IC₅₀ & Target	EC50: 20.8 nM (RORγt)^[1]
体内研究 (In Vivo)	RORγt agonist 1 shows high metabolic stability (t1/2 = 113 min) in mouse liver microsome and has improved aqueous solubility at pH 7.4^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	545.45
Formula	C₂₄H₁₇F₆NO₅S
CAS 号	2377378-89-5
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]. Zhu Y, et al. Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists. Eur J Med Chem. 2019 Aug 6;182:111589.

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VDR agonist 1

发表于2023年8月7日由上海金畔生物科技有限公司

VDR agonist 1

VDR agonist 1 (compound 28) 是一种非甾体类维生素 D 受体 (VDR) 的激动剂，在MCF-7 细胞中测得其 IC₅₀ 值为 690 nM。VDR agonist 1 通过上调 p21 和 p27 的表达来抑制细胞周期，通过增加 BAX 的表达来促进细胞凋亡，降低 Bcl-2 的表达。

VDR agonist 1 Chemical Structure

CAS No. : 2269494-43-9

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生物活性	VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC₅₀ of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2^[1].
IC₅₀ & Target	IC50: 690 nM (VDR in MCF-7 cells)^[1].
分子量	509.77
Formula	C₃₂H₅₁N₃O₂
CAS 号	2269494-43-9
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]. Wang C, et al. Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer. Eur J Med Chem. 2019 Feb 1;163:787-803.

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STING agonist-3 trihydrochloride

发表于2023年7月20日由上海金畔生物科技有限公司

STING agonist-3 trihydrochloride

STING agonist-3 trihydrochloride 源于专利 WO2017175147A1 (实施例10)，是一种选择性和非核苷酸的小分子 STING 激动剂，pEC₅₀ 和 pIC₅₀ 分别为 7.5 和 9.5。STING agonist-3 trihydrochloride 具有持久的抗肿瘤作用，并且在改善癌症研究方面具有巨大潜力。

STING agonist-3 trihydrochloride Chemical Structure

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STING agonist-3 trihydrochloride 的其他形式现货产品:

STING agonist-3

生物活性	STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC₅₀ and pEC₅₀ of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer^[1].
IC₅₀ & Target	STING^[1]
体外研究 (In Vitro)	STING agonist-3 trihydrochloride exhibits a pEC₅₀ value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter^[1]. STING agonist-3 trihydrochloride exhibits a pIC₅₀ value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	860.19
Formula	C₃₇H₄₅Cl₃N₁₂O₆
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]. Adam Kenneth, et al. Heterocyclic amides useful as protein modulators.patent WO2017175147A1

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Wnt/β-catenin agonist 1

发表于2023年7月20日由上海金畔生物科技有限公司

Wnt/β-catenin agonist 1

Wnt/β-catenin agonist 1 (compound 3f) 是 Wnt/β-catenin 信号通路的一个激动剂，EC₅₀ 值为 0.27 μM。

Wnt/β-catenin agonist 1 Chemical Structure

CAS No. : 2305372-67-0

规格	价格	是否有货
5 mg	￥4500	询问价格 & 货期
10 mg	￥7200	询问价格 & 货期
25 mg	￥14600	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	Wnt/β-catenin agonist 1 (compound 3f) is a Wnt/β-catenin signalling pathway agonist, with an EC₅₀ of 0.27 μM^[1].
体外研究 (In Vitro)	EC50: 0.27 μM (Wnt/β-catenin)^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	363.45
Formula	C₂₂H₂₅N₃O₂
CAS 号	2305372-67-0
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]. Chen DZ, et al. Design, synthesis and structure-activity relationship optimization of phenanthridine derivatives as new Wnt/β-catenin signalling pathway agonists. Bioorg Chem. 2019 Mar;84:285-294.

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TLR7/8 agonist 4

发表于2023年6月5日由上海金畔生物科技有限公司

TLR7/8 agonist 4

TLR7/8 agonist 4 (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 Chemical Structure

CAS No. : 2388520-33-8

规格		是否有货
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生物活性

TLR7/8 agonist 4 (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

324.42

Formula

C₁₈H₂₄N₆

CAS 号

2388520-33-8

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

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TLR7/8 agonist 4 hydroxy-PEG10-acid

发表于2023年6月5日由上海金畔生物科技有限公司

TLR7/8 agonist 4 hydroxy-PEG10-acid

TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) 是抗体-药物偶联物的一部分，由 TLR7/8 激活剂 TLR7/8 agonist 4 (HY-139018) 和可降解的 ADC linker hydroxy-PEG10-acid (HY-133307) 连接而成。

TLR7/8 agonist 4 hydroxy-PEG10-acid Chemical Structure

CAS No. : 2388520-17-8

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生物活性

TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307)^[1].

IC₅₀ & Target^[1]

Traditional Cytotoxic Agents

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

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

分子量

837.01

Formula

C₄₁H₆₈N₆O₁₂

CAS 号

2388520-17-8

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]. Shelley Erin ACKERMAN, et al. Immunoconjugates targeting her2. WO2020190725A1.

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STING agonist-4

发表于2023年5月25日由上海金畔生物科技有限公司

STING agonist-4 纯度: 98.08%

STING agonist-4 是干扰素基因 (STING) 的受体激动剂的刺激剂，它的表观抑制常数 IC₅₀ 为 20 nM，STING agonist-4 是一种含两个对称相关的氨基苯并咪唑 (ABZI) 基的化合物。

STING agonist-4 Chemical Structure

CAS No. : 2138300-40-8

规格	价格	是否有货
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg	￥15000	In-stock
100 mg	￥21000	In-stock
200 mg		询价
500 mg		询价

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STING agonist-4 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC₅₀) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function^[1].

IC₅₀ & Target

IC50: 20 nM (STING agonist-4)^[1]

体外研究
(In Vitro)

STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC₅₀ of 3.1 μM^[1].
STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (K_d) of approximately 1.6 nM^[1].
STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC₅₀ of 53.9 μM^[1].
STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1^[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:	Human peripheral blood mononuclear cells (PBMCs)
Concentration:	0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM
Incubation Time:	2 hours
Result:	Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β.

分子量

678.74

Formula

C₃₄H₃₈N₁₂O₄

CAS 号

2138300-40-8

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 : 10 mg/mL (14.73 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

*STING agonist-4 is usually formulated as a suspension.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4733 mL	7.3666 mL	14.7332 mL
5 mM	0.2947 mL	1.4733 mL	2.9466 mL
10 mM	0.1473 mL	0.7367 mL	1.4733 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 (1.47 mM); Suspended solution; Need ultrasonic

此方案可获得 1 mg/mL (1.47 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 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 (1.47 mM); Suspended solution; Need ultrasonic

此方案可获得 1 mg/mL (1.47 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 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

*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]. Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.

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标签归档：agonist

STING agonist-7

TLX agonist 1

TLX agonist 1 相关产品

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diABZI STING agonist-1 trihydrochloride

diABZI STING agonist-1 trihydrochloride 相关产品

•相关化合物库:

BMP signaling agonist sb4

BMP signaling agonist sb4 相关产品

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STING agonist-3

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1V209(Synonyms: TLR7 agonist T7)

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STING agonist-3 trihydrochloride

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STING agonist-4

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