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.
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Farnesoid X Receptor Products |
|---|
| ASC-42
ASC-42 is a novel, potentially best-in-class, highly potent and selective non-steroidal FXR agonist that also inhibits the transcription of HBV RNA to hepatitis B surface antigen by inhibiting the transcription of HBV covalent closed-circle DNA (cccDNA) to HBV RNA. |
| Linafexor
Linafexor is a bile acid receptor (FXR) agonist that may be used in studies related to cholangitis and non-alcoholic steatohepatitis. |
| MET-409
MET-409 is an oral non-steroidal bile acid receptor FXR agonist for studies related to inflammatory bowel disease and irritable bowel syndrome. |
| FXR agonist 5
FXR agonist 5 is a FXR agonist. |
| XJ02862-S2
XJ02862-S2 shows potent FXR agonistic activity. |
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