| Bioactivity | 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]. | ||||||||||||
| 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) | ||||||||||||
| Invitro | 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]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | EDP-305 | ||||||||||||
| CAS | 1933507-63-1 | ||||||||||||
| Formula | C36H58N2O5S | ||||||||||||
| Molar Mass | 630.92 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Erstad DJ, et al. Molecular magnetic resonance imaging accurately measures the antifibrotic effect of EDP-305, a novel farnesoid X receptor agonist. Hepatol Commun. 2018 May 21;2(7):821-835. [2]. Chau M, et al. Characterization of EDP-305, a Highly Potent and Selective Farnesoid X Receptor Agonist, for the Treatment of Non-alcoholic Steatohepatitis[J]. International Journal of Gastroenterology, 2019(1). |
EDP-305
CAS: 1933507-63-1 F: C36H58N2O5S W: 630.92
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeri
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