Free shipping on all orders over $ 500


Cat. No. M2018
GW4064 Structure

GW 4064

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 54  USD60 In stock
5mg USD 42.3  USD47 In stock
10mg USD 70.2  USD78 In stock
50mg USD 237.6  USD264 In stock
100mg USD 437.4  USD486 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

Product Citations
Customer Product Validations & Biological Datas
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
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 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.

Chemical Information
Molecular Weight 542.84
Formula C28H22Cl3NO4
CAS Number 278779-30-9
Purity 99.62%
Solubility DMSO 89 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.

Related Farnesoid X Receptor Products

Gly-β-MCA is a potent, stable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor.


Vonafexor is a farnesoid X receptor agonist.


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.

Abmole Inhibitor Catalog 2017

Keywords: GW4064, GW 4064 supplier, Farnesoid X Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.