产品
编 号：F750932
分子式：C36H59NO5
分子量：585.86
分子式：C36H59NO5
分子量：585.86
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2295804-68-9
产品详情
生物活性：
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.
体内研究：
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.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.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.Animal Model:Adult male C57BL/6 mice (GAN (Gubra-amylin NASH)-diet induced NASH model).
Dosage:10 mg/kg
Administration:Oral administration; single daily for 12 weeks.
Result:Reversed metabolic dysfunction in GAN-induced NASH mice.Reduced GAN-diet-induced hepatic steatosis, injury, inflammation, and fibrosis.Inhibited the hepatic mRNA expression involved in lipid metabolism, inflammatory signaling, and fibrogenesis in GAN-diet-induced mice.Significantly antagonized intestinal FXR signaling and bile acid reabsorption.
Animal Model:Adult male C57BL/6 mice (HFMCD-diet induced NASH model).
Dosage:3, 10, 30 mg/kg
Administration:Oral administration; single daily for 4 weeks.
Result:Significantly decreased serum ALT and AST levels at 30 mg/kg, and markedly lowered the hepatic TG concentration in both 10 and 30 mg/kg.Lowered hepatic hydroxyproline level.
体外研究：
FXR antagonist 1 (0-100 μM; 24 h) shows FXR antagonistic activities in HEK293T cells.
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.
体内研究：
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.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.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.Animal Model:Adult male C57BL/6 mice (GAN (Gubra-amylin NASH)-diet induced NASH model).
Dosage:10 mg/kg
Administration:Oral administration; single daily for 12 weeks.
Result:Reversed metabolic dysfunction in GAN-induced NASH mice.Reduced GAN-diet-induced hepatic steatosis, injury, inflammation, and fibrosis.Inhibited the hepatic mRNA expression involved in lipid metabolism, inflammatory signaling, and fibrogenesis in GAN-diet-induced mice.Significantly antagonized intestinal FXR signaling and bile acid reabsorption.
Animal Model:Adult male C57BL/6 mice (HFMCD-diet induced NASH model).
Dosage:3, 10, 30 mg/kg
Administration:Oral administration; single daily for 4 weeks.
Result:Significantly decreased serum ALT and AST levels at 30 mg/kg, and markedly lowered the hepatic TG concentration in both 10 and 30 mg/kg.Lowered hepatic hydroxyproline level.
体外研究：
FXR antagonist 1 (0-100 μM; 24 h) shows FXR antagonistic activities in HEK293T cells.
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