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Cat. No. M2018
GW4064 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 300 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 542.84
Formula C28H22Cl3NO4
CAS Number 278779-30-9
Purity 99.62%
Solubility DMSO 100 mg/mL
Storage at -20°C

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.

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Keywords: GW4064 supplier, Farnesoid X Receptor, inhibitors

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