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PX20606

Chemical Structure : PX20606

CAS No.: 1268245-19-7

PX20606 (PX-102, PX102)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 554.85
Formula C29H22Cl3NO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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