产品
编 号：F762405
分子式：C36H58N2O5S
分子量：630.92
分子式：C36H58N2O5S
分子量：630.92
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1933507-63-1
产品详情
生物活性：
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
体内研究：
EDP‐305 (0-30 mg/kg, Oral gavage, daily for 2 weeks) reduces serum markers of liver injury, and reduces liver fibrosis in a dose-dependent manner in BDL rats.EDP‐305 (0-30 mg/kg, Oral gavage, daily for 6 weeks) reduces liver fibrosis in a dose-dependent manner in CDAHFD mice.Animal Model:Male CD rats (underwent BDL, n=24, n=8 for each group)
Dosage:0, 10 and 30 mg/kg
Administration:Oral gavage, daily, started on day 4 after BDL and continued until days 17-18
Result:Significantly reduced alanine aminotransferase and aspartate aminotransferase. Showed a dose-dependent reduction in CPA. Reduced hydroxyproline levels in whole liver tissue samples. Reduced messenger RNA (mRNA) relative quantification (RQ) for both Col1a1 and actin, alpha 2, smooth muscle, aorta (Acta2).
Animal Model:Male C57BL/6 mice (n = 24, fed a CDAHFD consisting of 60% kcal fat and 0.1% methionine)
Dosage:0, 10 and 30 mg/kg
Administration:Oral gavage, daily, started at the beginning of week 6 on the diet and were continued until week 12
Result:Reduced serum triglycerides, and significantly reduced hydroxyproline and MR liver signal intensity in a dose-dependent manner. Showed a dose‐dependent reduction in mRNA expression of lysyl oxidase genes Lox and Loxl1-4.
体外研究：
EDP‐305 (10 μM, 72 h) directly activates FXR in liver hepatoctyes but not stellate cells. EDP-305 (0-5 μM, 16 h) increases the expression of the FXR target gene, SHP, and downregulates CYP7A1 expression in HepaRG hepatocytes.
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
体内研究：
EDP‐305 (0-30 mg/kg, Oral gavage, daily for 2 weeks) reduces serum markers of liver injury, and reduces liver fibrosis in a dose-dependent manner in BDL rats.EDP‐305 (0-30 mg/kg, Oral gavage, daily for 6 weeks) reduces liver fibrosis in a dose-dependent manner in CDAHFD mice.Animal Model:Male CD rats (underwent BDL, n=24, n=8 for each group)
Dosage:0, 10 and 30 mg/kg
Administration:Oral gavage, daily, started on day 4 after BDL and continued until days 17-18
Result:Significantly reduced alanine aminotransferase and aspartate aminotransferase. Showed a dose-dependent reduction in CPA. Reduced hydroxyproline levels in whole liver tissue samples. Reduced messenger RNA (mRNA) relative quantification (RQ) for both Col1a1 and actin, alpha 2, smooth muscle, aorta (Acta2).
Animal Model:Male C57BL/6 mice (n = 24, fed a CDAHFD consisting of 60% kcal fat and 0.1% methionine)
Dosage:0, 10 and 30 mg/kg
Administration:Oral gavage, daily, started at the beginning of week 6 on the diet and were continued until week 12
Result:Reduced serum triglycerides, and significantly reduced hydroxyproline and MR liver signal intensity in a dose-dependent manner. Showed a dose‐dependent reduction in mRNA expression of lysyl oxidase genes Lox and Loxl1-4.
体外研究：
EDP‐305 (10 μM, 72 h) directly activates FXR in liver hepatoctyes but not stellate cells. EDP-305 (0-5 μM, 16 h) increases the expression of the FXR target gene, SHP, and downregulates CYP7A1 expression in HepaRG hepatocytes.
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