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GW 4064

Item № 10006611
CAS № 278779-30-9
Purity ≥95%
product image
                (CAS 278779-30-9)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $69.00 0.00
     10 mg $108.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

Description

Farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity.1 GW 4064 is a selective agonist of FXR (EC50 = 15 nM).2 It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.2 GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.3,4,5,6,7

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Technical Information
Formal Name
3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-benzoic acid
CAS Number
278779-30-9
Molecular Formula
C28H22Cl3NO4
Formula Weight
542.8
Purity
≥95%
Formulation
A crystalline solid
λmax
304 nm
SMILES
ClC(C=CC=C1Cl)=C1C2=NOC(C(C)C)=C2COC(C=C3)=CC(Cl)=C3/C=C/C4=CC(C(O)=O)=CC=C4
InChI Code
InChI=1S/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+
InChI Key
BYTNEISLBIENSA-MDZDMXLPSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

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References & Product Citations
Product Description References

1. Rader, D.J. Liver X receptor and farnesoid X receptor as therapeutic targets American Journal of Cardiology 100, 15N-19N (2007).

2. Maloney, P.R., Parks, D.J., Haffner, C.D., et al. Identification of a chemical tool for the orphan nuclear receptor FXR Journal of Medicinal Chemistry 43(16), 2971-2974 (2000).

3. Haeusler, R.A., Pratt-Hyatt, M., Welch, C.L., et al. Impaired generation of 12-hydroxylated bile acids links hepatic insulin signaling with dyslipidemia Cell Metabolism 15(1), 65-74 (2012).

4. Watanabe, M., Horai, Y., Houten, S.M., et al. Lowering bile acid pool size with a synthetic farnesoid X receptor (FXR) agonist induces obesity and diabetes through reduced energy expenditure The Journal of Biological Chemisty 286(30), 26913-26920 (2011).

5. Deuschle, U., Schüler, J., Schulz, A., et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model PLoS One 7(10), e43044 (2012).

6. Catalano, S., Malvindi, R., Giordano, C., et al. Farnesoid X receptor, through the binding with steroidogenic factor 1-responsive element, inhibits aromatase expression in tumor Leydig cells The Journal of Biological Chemisty 285(8), 5581-5593 (2010).

7. Cariou, B., van Harmelen, K., Duran-Sandoval, D., et al. The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice The Journal of Biological Chemisty 281(16), 11039-11049 (2006).

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