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GW 501516 (CAS 317318-70-0) LS-H3

PPAR delta agonist
LS-H3-1 / 1 mg / $185
LS-H3-5 / 5 mg / $205
LS-H3-10 / 10 mg / $245
USA Shipment Only
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Description: Peroxisome proliferator-activated receptor delta (PPAR delta) stimulation or over-expression in adipocytes leads to increased fatty acid oxidation, improved exercise tolerance, and resistance to obesity. GW 501516 is the first highly selective synthetic PPAR delta agonist available. GW 501516 binds to human PPAR delta with an IC50 value of 1 nM, and is at least 100-fold selective for PPAR delta compared to PPAR alpha and PPAR gamma . In obese primates, GW 501516 increases high density lipoprotein cholesterol and apolipoprotein A-1 specific reverse cholesterol transport. GW 501516 is therefore a model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism. H3_ChemicalStructureImage.png
2-[2-methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-acetic acid
GW1516
biochemical, chemical, agonist
LS-H3
317318-70-0
C21H18F3NO3S2
≥98%
A crystalline solid
 
OC(COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)C=C1C)=O
InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27)
YDBLKRPLXZNVNB-UHFFFAOYSA-N
Shipped at 4°C, store at -20°C, ≥ 2 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: PPARD / PPAR Delta related products

Usage Information

GW 501516 is supplied as a crystalline solid. A stock solution may be made by dissolving the GW 501516 in an organic solvent purged with an inert gas. GW 501516 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of GW 501516 in these solvents is approximately 12, 20, and 25 mg/ml, respectively. GW 501516 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, GW 501516 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. GW 501516 has a solubility of approximately 0.5 mg/ml in a 1:2 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Wang, Y.-X., Lee, C.-H., Tiep, S., et al. Peroxisome-proliferator-activated receptor δ activates fat metabolism to prevent obesity. Cell 113, 159-170 (2003).
  2. Sznaidman, M.L., Haffner, C.D., Maloney, P.R., et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ)-synthesis and biological activity. Bioorg. Medicinal Chem. Letters 13, 1517-1521 (2003).
  3. Oliver, W.R., Shenk, J.L., Snaith, M.R., et al. A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport. Proc. Natl. Acad. Sci. USA 98(9), 5306-5311 (2001).

 


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