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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Farnesoid X Receptor (FXR)-PX20606
PX20606

Chemical Structure : PX20606

CAS No.: 1268245-19-7

PX20606 (PX-102, PX102)

货号: PC-26702Not For Human Use, Lab Use Only.

PX20606 (PX-102) is a potent, selective FXR agonist with EC50 of 771 nM, 237 nM and 129 nM for mouse, rat, and human FXR in biochemical TR-FRET assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PX20606 (PX-102) is a potent, selective FXR agonist with EC50 of 771 nM, 237 nM and 129 nM for mouse, rat, and human FXR in biochemical TR-FRET assays.
PX20606 (PX-102) has EC50 of 268, 179, 107 and 77 nM in GAL4-FXR-LBD fusion cellular reporter assays using mouse, rat, monkey, and human FXR-LBDs.
PX20606 potently lowered total cholesterol and, despite the observed HDL cholesterol (HDLc) reduction, caused a highly significant decrease in atherosclerotic plaque size, in CETPtg-LDLR(−/−) mice.
PX20606 reduced total cholesterol, specifically lowered HDL2c but not HDL3c or apolipoprotein A1, in normolipidemic cynomolgus monkeys. ameliorates portal hypertension by targeting vascular remodelling and sinusoidal dysfunction.

物理化学性质&存储条件

分子量 554.85
分子式 C29H22Cl3NO4
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

10 mM in DMSO

Chemical Name/SMILES

4-[2-[2-chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]phenyl]cyclopropyl]benzoic acid

参考文献

1. Hambruch E, et al. J Pharmacol Exp Ther. 2012 Dec;343(3):556-67.

2. Schwabl P, et al. J Hepatol. 2017 Apr;66(4):724-733.

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