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首页-小分子抑制剂&激动剂-GPCR-TGR5 (GPCR19, GPR131, GPBAR1)-BAR501
BAR501

Chemical Structure : BAR501

CAS No.: 1632118-69-4

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BAR501 (BAR 501;BAR-501)

货号: PC-42345Not For Human Use, Lab Use Only.

BAR501 is a potent, selective GPBAR1 (GPCR19, TGR5) agonist devoid of any FXR agonistic activity, effectively transactivates GPBAR1 in HEK293 cells with EC50 of 1 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAR501 is a potent, selective GPBAR1 (GPCR19, TGR5) agonist devoid of any FXR agonistic activity, effectively transactivates GPBAR1 in HEK293 cells with EC50 of 1 uM.
BAR501 effectively reduces hepatic perfusion pressure and counteracts the vasoconstriction activity of norepinephrine in rats, effectively protects against development of endothelial dysfunction by increasing liver CSE expression and activity and by reducing endothelin (ET)-1 gene expression in CCl4 models.

物理化学性质&存储条件

分子量 406.64164
分子式 C26H46O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 10 mM
Chemical Name/SMILES

Cholane-3,7,24-triol, 6-ethyl-, (3α,5β,6β,7β)-

参考文献

1. Renga B, et al. PLoS One. 2015 Nov 5;10(11):e0141082.

2. Biagioli M, et al. J Immunol. 2017 Jul 15;199(2):718-733.

3. Carino A, et al. Sci Rep. 2017 Oct 20;7(1):13689.

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