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.
|Source||World J Gastroenterol (2014). Figure 1. GW4064|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
Bile acid receptor agonist GW4064 regulates PPARγ coactivator-1α expression through estrogen receptor-related receptor α.
Dwivedi SK, et al. Mol Endocrinol. 2011 Jun;25(6):922-32. PMID: 21493670.
The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice.
Cariou B, et al. J Biol Chem. 2006 Apr 21;281(16):11039-49. PMID: 16446356.
Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis.
Liu Y, et al. J Clin Invest. 2003 Dec;112(11):1678-87. PMID: 14623915.
|Related Farnesoid X Receptor Products|
Z-Guggulsterone is a mineralocorticoid, progesterone and glucocorticoid receptor antagonist (Ki values are 37, 224 and 252 nM respectively) and weak androgen receptor agonist (Ki = 315 nM).
DY268 is a potent FXR antagonist with IC50 of 7.5 nM.
Nidufexor is a farnesoid X receptor (FXR) agonist.
Cilofexor is a farnesoid X receptor (FXR) agonist.
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.