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EDP-305

Cat. No. M22512

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EDP-305 Structure
Synonym:

EDP305

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Quality Control & Documentation
Biological Activity

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 can be used for the research of primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH). 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 (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.

Chemical Information
Molecular Weight 630.92
Formula C36H58N2O5S
CAS Number 1933507-63-1
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Alaa Ahmad, et al. Clin Transl Sci. Assessment of drug-drug interaction potential with EDP-305, a farnesoid X receptor agonist, in healthy subjects

[2] Vlad Ratziu, et al. J Hepatol. EDP-305 in patients with NASH: A phase II double-blind placebo-controlled dose-ranging study

[3] Claus Kremoser. J Hepatol. FXR agonists for NASH: How are they different and what difference do they make?

[4] Ping An, et al. Liver Int. A novel non-bile acid FXR agonist EDP-305 potently suppresses liver injury and fibrosis without worsening of ductular reaction

[5] Shen Li, et al. FASEB J. The farnesoid X receptor agonist EDP-305 reduces interstitial renal fibrosis in a mouse model of unilateral ureteral obstruction

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Keywords: EDP-305, EDP305 supplier, Farnesoid X Receptor, inhibitors, activators

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