1. Metabolic Enzyme/Protease
  2. FXR
    Phosphatase
    Cytochrome P450
  3. EDP-305

EDP-305 

Cat. No.: HY-134988 Purity: 96.01%
Handling Instructions

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.

For research use only. We do not sell to patients.

EDP-305 Chemical Structure

EDP-305 Chemical Structure

CAS No. : 1933507-63-1

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target

IC50: 8 ± 3 nM (Full-length FXR in HEK cells), 34 ± 8 nM (Chimeric FXR in CHO cells), >15000 nM (TGR5 in CHO cells)[2]

In Vitro

EDP‐305 (10 μM, 72 h) directly activates FXR in liver hepatoctyes but not stellate cells[1].
EDP-305 (0-5 μM, 16 h) increases the expression of the FXR target gene, SHP, and downregulates CYP7A1 expression in HepaRG hepatocytes[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Hepatic stellate cell (HSC) lines, primary HSCs and hepatocytes
Concentration: 10 μM
Incubation Time: 72 h
Result: Induced mRNA expression of SHP and FGF19 in human hepatocytes, and elicited no induction of downstream targets SHP or FGF15/19 in stellate lines.

RT-PCR[2]

Cell Line: HepaRG hepatocytes
Concentration: 0.05, 0.1, 0.5, 1, 5, 10, 50, 100, 500, 1000, 5000 nM
Incubation Time: 16 h
Result: Dose-dependently increased the expression of the FXR target gene, SHP, and downregulated CYP7A1 expression in HepaRG hepatocytes.
In Vivo

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[1].
EDP‐305 (0-30 mg/kg, Oral gavage, daily for 6 weeks) reduces liver fibrosis in a dose-dependent manner in CDAHFD mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD rats (underwent BDL, n=24, n=8 for each group)[1]
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)[1]
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.
Molecular Weight

630.92

Formula

C36H58N2O5S

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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Product Name:
EDP-305
Cat. No.:
HY-134988
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