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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 |
| Related Farnesoid X Receptor Products |
|---|
| GW4064
GW4064 is a selective, non-steroidal agonist of the orphan nuclear receptor FXR with EC50 of 15 nM. |
| WAY-362450 (Turofexorate isopropyl)
WAY-362450 (Turofexorate isopropyl; XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM. |
| Chenodeoxycholic acid
Chenodeoxycholic acid is an epimer of ursodeoxycholic acid, which inhibits the production of cholesterol in the liver and absorption in the intestines. |
| Obeticholic Acid (INT-747)
Obeticholic Acid (INT-747) is a potent, orally active, selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.May be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Sevelamer HCl
Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption. |
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