The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis.
Eur J Pharmacol. 2024 Mar 5;966:176334.
Farnesoid X receptor agonist tropifexor detoxifies ammonia by regulating the glutamine metabolism and urea cycles in cholestatic livers
Tropifexor purchased from AbMole
Liver Int. 2021 Sep;41(9):2117-2131.
A nonbile acid farnesoid X receptor agonist tropifexor potently inhibits cholestatic liver injury and fibrosis by modulating the gut-liver axis
Tropifexor purchased from AbMole
Molecular Weight | 603.58 |
Formula | C29H25F4N3O5S |
CAS Number | 1383816-29-2 |
Solubility (25°C) | 10 mM in DMSO |
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 |
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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. |
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FXR agonist 5 is a FXR agonist. |
XJ02862-S2
XJ02862-S2 shows potent FXR agonistic activity. |
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