Fexaramine is a selective farnesoid X receptor (FXR) agonist with EC50 of 25 nM, with 100-fold increased affinity relative to natural compounds.
Fexaramine significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and β-catenin signaling. By mimicking this tissue-selective effect, the gut-restricted FXR agonist fexaramine (Fex) robustly induces enteric fibroblast growth factor 15 (FGF15), leading to alterations in BA composition, but does so without activating FXR target genes in the liver.
Fexaramine treatment of DIO mice produces a striking metabolic profile that includes reduced weight gain, decreased inflammation, browning of WAT and increased insulin sensitization.
| Molecular Weight | 496.64 |
| Formula | C32H36N2O3 |
| CAS Number | 574013-66-4 |
| Solubility (25°C) | DMSO 50 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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