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GW 9578

Item № 10011211
CAS № 247923-29-1
Purity ≥98%
product image
                (CAS 247923-29-1)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     500 µg $23.00 0.00
     1 mg $44.00 0.00
     5 mg $184.00 0.00
     10 mg $322.00 0.00

Pricing updated 2019-07-23. Prices are subject to change without notice.

Description

Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.1,2 Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. 3 GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.4 GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.4 GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.4 Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.5

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Technical Information
Formal Name
2-[[4-[2-[[[(2,4-difluorophenyl)amino]carbonyl]heptylamino]ethyl]phenyl]thio]-2-methyl-propanoic acid
CAS Number
247923-29-1
Molecular Formula
C26H34F2N2O3S
Formula Weight
492.6
Purity
≥98%
Formulation
A solution in methyl acetate
λmax
231, 268 nm
SMILES
CCCCCCCN(CCc1ccc(cc1)SC(C)(C)C(=O)O)C(=O)Nc1ccc(F)cc1F
InChI Code
InChI=1S/C26H34F2N2O3S/c1-4-5-6-7-8-16-30(25(33)29-23-14-11-20(27)18-22(23)28)17-15-19-9-12-21(13-10-19)34-26(2,3)24(31)32/h9-14,18H,4-8,15-17H2,1-3H3,(H,29,33)(H,31,32)
InChI Key
KYQNYMXQHLMADB-UHFFFAOYSA-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
≥ 1 year
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Additional Information

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References & Product Citations
Product Description References

1. Latruffe, N., and Vamecq, J. Peroxisome proliferators and peroxisome proliferator activated receptors (PPARs) as regulators of lipid metabolism Biochimie 79, 81-94 (1997).

2. Lemberger, T., Desvergne, B., and Wahli, W. Peroxisome proliferator-activated receptors: A nuclear receptor signaling pathway in lipid physiology Annual Reviews of Cell Development and Biology 12, 335-363 (1996).

3. Mandard, S., Müller, M., and Kersten, S. Peroxisome proliferator-activated receptor α target genes Cellular and Molecular Life Sciences 61, 393-416 (2004).

4. Brown, P.J., Winegar, D.A., Plunket, K.D., et al. A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARα agonist with potent lipid-lowering activity Journal of Medicinal Chemistry 42, 3785-3788 (1999).

5. Guerre-Millo, M., Gervois, P., Raspé, E., et al. Peroxisome proliferator-activated receptor α activators improve insulin sensitivity and reduce adiposity The Journal of Biological Chemisty 275, 16638-16642 (2000).

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