For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I043467 |
| CAS Number | 1933507-63-1 |
| Synonyms | 1-(4-tert-butylphenyl)sulfonyl-3-[(3R)-3-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]butyl]urea |
| Molecular Formula | C36H58N2O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C36H58N2O5S/c1-8-26-30-21-24(39)15-18-36(30,7)29-16-19-35(6)27(13-14-28(35)31(29)32(26)40)22(2)17-20-37-33(41)38-44(42,43)25-11-9-23(10-12-25)34(3,4)5/h9-12,22,24,26-32,39-40H,8,13-21H2,1-7H3,(H2,37,38,41)/t22-,24-,26-,27-,28+,29+,30+,31+,32-,35-,36-/m1/s1 |
| InChIKey | SJKLCUGQVVYDCX-HRNVLBFRSA-N |
| SMILES | CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCNC(=O)NS(=O)(=O)C5=CC=C(C=C5)C(C)(C)C)C)C)O |
| 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). |
