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GW 9578 (CAS 247923-29-1) LS-H56

PPAR alpha agonist
LS-H56-500 / 500 µg / $175
LS-H56-1000 / 1000 µg / $195
LS-H56-5000 / 5000 µg / $285
LS-H56-10000 / 10000 µg / $385
USA Shipment Only
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Description: Peroxisome proliferator-activated receptor alpha (PPAR alpha) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis. Activation of PPAR alpha results in expression of a variety of genes, particularly those involved in fatty acid beta -oxidation, binding, and transport. GW 9578 is a potent agonist of PPAR alpha that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively. GW 9578 is highly selective for PPAR alpha compared to PPAR gamma and PPAR delta, 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. 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. Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls. H56_ChemicalStructureImage.png
2-[[4-[2-[[[(2,4-difluorophenyl)amino]carbonyl]heptylamino]ethyl]phenyl]thio]-2-methyl-propanoic acid
 
biochemical, chemical, agonist
LS-H56
247923-29-1
C26H34F2N2O3S
≥98%
A solution in methyl acetate
 
CCCCCCCN(CCc1ccc(cc1)SC(C)(C)C(=O)O)C(=O)Nc1ccc(F)cc1F
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)
KYQNYMXQHLMADB-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 1 year shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: PPARA / PPAR Alpha related products

Usage Information

GW 9578 is supplied as a solution in methyl acetate. To change the solvent, simply evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice. Solvents such as ethanol, DMSO, and dimethyl formamide (DMF) purged with an inert gas can be used. The solubility of GW 9578 in ethanol is approximately 2.5 mg/ml and approxmately 10 mg/ml in DMSO and DMF. GW 9578 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, the methyl acetate solution of GW 9578 should be diluted with the aqueous buffer of choice. GW 9578 has a solubility of approximately 0.3 mg/ml in a 1:2 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

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. Annu. Rev. Cell Dev. Biol. 12, 335-363 (1996).
  3. Mandard, S., Müller, M., and Kersten, S. Peroxisome proliferator-activated receptor a target genes. Cell. Mol. Life Sci. 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 PPARa agonist with potent lipid-lowering activity. J. Med. Chem. 42, 3785-3788 (1999).
  5. Guerre-Millo, M., Gervois, P., Raspé, E., et al. Peroxisome proliferator-activated receptor a activators improve insulin sensitivity and reduce adiposity. J. Biol. Chem. 275, 16638-16642 (2000).

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