SML1491

GW501516

≥98% (HPLC), PPARδ agonist, powder

• Synonym(s): 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-acetic acid, GW1516
• Empirical Formula (Hill Notation): C₂₁H₁₈F₃NO₃S₂
• CAS Number: 317318-70-0
• Molecular Weight: 453.50
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825917
• NACRES: NA.77
• MDL number: MFCD09033000
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Product Name: GW501516, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: −20°C
• SMILES string: FC(F)(F)c1ccc(cc1)c2[s]c(c(n2)C)CSc3cc(c(cc3)OCC(=O)O)C
• 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)
• InChI key: YDBLKRPLXZNVNB-UHFFFAOYSA-N

Description

Application

GW501516 has been used as a peroxisome proliferator-activated receptor (PPAR) δ agonist:

• to treat the differentiated L6 myotubes to test its effect on free fatty acid (FFA) uptake under mild hypoxia conditions
• in organoid culture medium to test its effect on self-renewal of PR domain containing 16 (Prdm16)-depleted intestinal stem cells
• as a component in the defatting medium for primary human hepatocytes (PHH) culture

GW501516 has been used to study its effect on mutation-driven colorectal tumorigenesis and tumor invasion using mouse model.

Biochem/physiol Actions

GW501516 is a selective Peroxisome Proliferator-Activated Receptor delta (PPARδ) agonist with high affinity (Ki = 1 nM) and potency (EC₅₀ = 1 nM) for PPARδ and > 1000 fold selectivity over PPARα and PPARγ. GW501516 was shown to activate some of the same pathways activated through exercise, and was investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. However, GW501516 also showed an increase in cancer in rats.

GW501516 is a selective Peroxisome Proliferator-Activated Receptor delta (PPARδ) agonist.

PPARδ activation by GW501516, retards weight gain through fatty acid catabolism in adipose tissue and skeletal muscles. GW501516 causes an increase in the levels high-density lipoprotein cholesterol and apolipoprotein A (apoA) and reduction in the low density-lipoprotein cholesterol, apoB, and triglyceride.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable