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GW4064

Cat. No. M2018

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GW4064 Structure
Synonym:

GW 4064

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 47  USD47 In stock
10mg USD 78  USD78 In stock
50mg USD 264  USD264 In stock
100mg USD 486  USD486 In stock
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Quality Control & Documentation
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
Chemical Information
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
References

[1] Dwivedi SK, et al. Mol Endocrinol. Bile acid receptor agonist GW4064 regulates PPARγ coactivator-1α expression through estrogen receptor-related receptor α.

[2] Cariou B, et al. J Biol Chem. The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice.

[3] Liu Y, et al. J Clin Invest. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis.

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

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