FXR antagonist 1_product_DataBase

Bioactivity	FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies[1].
Invitro	FXR antagonist 1 (0-100 µM; 24 h) shows FXR antagonistic activities in HEK293T cells[1]. Cell Viability Assay[1] Cell Line:
In Vivo	FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) reduces adiposity and improves glucose sensitivity and ameliorates the progress of NASH in GAN-diet-induced NASH mice[1].FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) inhibits intestinal FXR Signaling but indirectly activates hepatic FXR signaling in GAN-diet-induced mice[1].FXR antagonist 1 (3, 10, 30 mg/kg; p.o.; single daily for 4 weeks) dose-dependently alleviates NASH pathologies in HFMCD-diet-induced mice[1]. Animal Model:
Name	FXR antagonist 1
CAS	2295804-68-9
Formula	C36H59NO5
Molar Mass	585.86
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Zhang C, et al. Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis. J Med Chem. 2022 Sep 15.

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