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GW4064 is a FXR agonist. There is no activity of GW4064 at other nuclear receptors at concentrations up to 1 μM. Treatment of differentiated 3T3-L1 adipocytes with the FXR-specific synthetic agonist GW4064 enhanced insulin signaling and insulin-stimulated glucose uptake. Finally, treatment with GW4064 improved insulin resistance in genetically obese ob/ob mice in vivo. Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg.
Protein Cell. 2024 Apr 18.
Gut dysbiosis impairs intestinal renewal and lipid absorption in Scarb2 deficiency-associated neurodegeneration
GW4064 purchased from AbMole
Gut Microbes. 2023 Jan-Dec;15(1):2221098.
Deletion of hepatic growth hormone receptor (GHR) alters the mouse gut microbiota by affecting bile acid metabolism
GW4064 purchased from AbMole
BMC Med. 2021 Apr 7;19(1):87.
Dexamethasone induces an imbalanced fetal-placental-maternal bile acid circulation: involvement of placental transporters
GW4064 purchased from AbMole
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Source | World J Gastroenterol (2014). Figure 1. GW4064 |
| Method | i.v. | |
| Cell Lines | Mice | |
| Concentrations | 2 μmol/L | |
| Incubation Time | 7 d | |
| Results | Treatment with the FXR agonist GW4064 also significantly decreased serum ALT and AST levels in HF diet-fed mice treated with LPS, further suggesting that FXR may have a protective role against liver injury in this NAFLD model |
| Molecular Weight | 542.84 |
| Formula | C28H22Cl3NO4 |
| CAS Number | 278779-30-9 |
| Solubility (25°C) | DMSO 89 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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