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Cat. No. Product Name CAS No. Information
PC-61390

Nidufexor

1773489-72-7

Nidufexor (LMB763, LMB-763) is a novel potent farnesoid X receptor (FXR) agonist for the treatment of non-alcoholic steatohepatitis (NASH) and hepatobiliary disorders.

PC-61368

Cilofexor

1418274-28-8

Cilofexor (GS-9674, GS9674, PX-104) is a novel specific, non-steroidal farnesoid X receptor (FXR) agonist that reduces liver fibrosis and ameliorates portal hypertension in rat NASH models.

Steatohepatitis

Phase 2 Clinical

PC-60080

GSK-2324

1020567-30-9

GSK-2324 (GSK2324) is a potent, selective, full FXR agonist with EC50 of 120 nM in FRET assay; lowers body weight gain and serum glucose in a DIO mouse model of diabetes.

PC-60056

Tropifexor

1383816-29-2

Tropifexor (LJN-452, LJN452) is a novel highly potent, selective, orally acitive FXR full agonist with EC50 of 0.26 nM; shows no significant off-target activity (>10,000-fold selectivity for FXR) in a panel of targets, including TGR5 (>10 uM); demonstratesin vivo activity in rodent PD models, and shows potential for treatment of cholestatic liver diseases and NASH.

Steatohepatitis

Phase 2 Clinical

PC-42924

INT-747

459789-99-2

INT-747(Obeticholic acid, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective FXR agonist (EC50=99 nM); possesses anticholeretic activity in rat model of cholestasis.

Other Indication

Approved

PC-43034

INT-767

1000403-03-1 INT-767 is a potent, selective, dual farnesoid X receptor (FXR) and TGR5 agonist with EC50 of 30 and 630 nM, respectively; fails to activate 15 other nuclear receptors involved in metabolic pathways, and does not inhibit cytochrome P450 enzymes; induces FXR-dependent lipid uptake by adipocytes and promotes TGR5-dependent glucagon-like peptide-1 (GLP-1) secretion by enteroendocrine cells; markedly decreases cholesterol and triglyceride levels in diabetic db/db mice.

Fibrosis

Phase 1 Clinical

PC-63021

MFA-1

139755-30-9 MFA-1 (Merck FXR agonist 1) is a potent, synthetic FXR agonist with EC50 of 16.9 nM in coactivator recruitment assays, displays 500-fold more potent than CDCA; displays an unexpected mode of binding and activation to FXR.

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