SML1491

Sigma-Aldrich

GW501516

≥98% (HPLC)

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:
Molecular Weight:
453.50
MDL number:
PubChem Substance ID:
Pricing and availability is not currently available.

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−20°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

Application

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

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

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.
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.

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis
Certificate of Origin
Activation of peroxisome proliferator-activated receptor-δ by GW501516 prevents fatty acid-induced nuclear factor-κB activation and insulin resistance in skeletal muscle cells.
Coll T, et al.
Endocrinology, 151(4), 1560-1569 (2010)
Pleotropic effects of PPARD accelerate colorectal tumor progression and invasion.
Liu Y, et al.
bioRxiv, 325001-325001 (2018)
Lipid effects of peroxisome proliferator-activated receptor-δ agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.
Olson E J, et al.
Arteriosclerosis, Thrombosis, and Vascular Biology, 32(9), 2289-2294 (2012)
Yi Ling Low et al.
Molecular pharmaceutics, 17(3), 873-884 (2020-01-17)
Brain levels of docosahexaenoic acid (DHA), an essential cognitively beneficial fatty acid, are reduced in Alzheimer's disease (AD). We have demonstrated in an AD mouse model that this is associated with reduced blood-brain barrier (BBB) transport of DHA and lower...
Buqing Ye et al.
The EMBO journal, 39(13), e103786-e103786 (2020-05-26)
Lgr5+ intestinal stem cells (ISCs) exhibit self-renewal and differentiation features under homeostatic conditions, but the mechanisms controlling Lgr5 + ISC self-renewal remain elusive. Here, we show that the chromatin remodeler SRCAP is highly expressed in mouse intestinal epithelium and ISCs. Srcap deletion...

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