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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
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Source | Liver Int (2021). Figure 4. Tropifexor (Abmole Bioscience) |
| Method | gavage | |
| Cell Lines | Guangxi Bama mini-pigs | |
| Concentrations | 1.06 μg/kg | |
| Incubation Time | a day since 2 d | |
| Results | RT-qPCR analysis showed that the mRNA levels of the cholangiocyte markers KRT7, KRT19 and MMP7 were reduced in BDL + TXR piglets compared with BDL piglets. Western blot analysis showed that the expression of CK19 protein was significantly decreased in the liver samples of BDL + TXR compared with that of BDL piglets. |
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Source | Liver Int (2021). Figure 3. Tropifexor (Abmole Bioscience) |
| Method | gavage | |
| Cell Lines | Guangxi Bama mini-pigs | |
| Concentrations | 1.06 μg/kg | |
| Incubation Time | a day since 2 d | |
| Results | Consistently, western blot analysis showed that BDL significantly increased the protein levels of α-SMA and collagen I in the liver samples of BDL piglets but not in that of BDL + TXR piglets |
| 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 |
| Related Farnesoid X Receptor Products |
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| ZLY28
ZLY28 is a first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 is also a novel anti-NASH agent. |
| 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. |
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