Cilofexor

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cilofexor (GS-9674、GS9674、PX-104) 是一种新型特异性非甾体法尼醇 X 受体 (FXR) 激动剂，可减少大鼠 NASH 模型中的肝纤维化并改善门静脉高压。

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(In Vivo):Cilofexor (GS-9674; 30 mg/kg; oral gavage; once daily; for 10 weeks; male Wistar rats) treatment significantly increases Fgf15 expression in the ileum and decreased Cyp7a1 in the liver in nonalcoholic steatohepatitis (NASH) rats. Liver fibrosis and hepatic collagen expression are significantly reduced. Cilofexor also significantly reduces hepatic stellate cell (HSC) activation and significantly decreases portal pressure, without affecting systemic hemodynamics.

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Animal Model:Male Wistar rats received a choline-deficient high fat diet (CDHFD)Dosage:30 mg/kg Administration:Oral gavage; once daily; for 10 weeks Result:Significantly increased Fgf15 expression in the ileum and decreased Cyp7a1 in the liver. Liver fibrosis and hepatic collagen expression were significantly reduced.

GS-9674 | GS9674 | PX-104

Metabolic Enzyme/Protease

FXR

FXR

Other Indications

Steatohepatitis

1418274-28-8

586.85

C28H22Cl3N3O5

>98% (HPLC)

DMSO : 125 mg/mL213.00 mM; H2O : < 0.1 mg/mL

OC(C1=CC=NC(N2CC(O)(C2)C3=C(C=C(C=C3)OCC4=C(ON=C4C5=C(C=CC=C5Cl)Cl)C6CC6)Cl)=C1)=O

2-[3-[2-Chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]phenyl]-3-hydroxy-1-azetidinyl]-4-pyridinecarboxylic acid

(-20℃)

With Ice Pack

≥ 2 years