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Cilofexor

SKU: orb1226325

Description

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.

Images & Validation

Key Properties

CAS Number1418274-28-8
MW586.85
Purity>98% (HPLC)
FormulaC28H22Cl3N3O5
SMILESOC(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
TargetFXR
SolubilityDMSO : 125 mg/mL213.00 mM; H2O : < 0.1 mg/mL

Bioactivity

In Vivo
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

GS-9674 | GS9674 | PX-104

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Protocol Information

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2 mg
$ 120.00
5 mg
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10 mg
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25 mg
$ 630.00
50 mg
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100 mg
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500 mg
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