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SML1491

Sigma-Aldrich

GW501516

≥98% (HPLC)

Synonyme(s) :

2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-acetic acid, GW1516

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About This Item

Formule empirique (notation de Hill):
C21H18F3NO3S2
Numéro CAS:
317318-70-0
Poids moléculaire :
453.50
Numéro MDL:
MFCD09033000
Code UNSPSC :
12352200
ID de substance PubChem :
329825917
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 20 mg/mL, clear

Température de stockage

−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)

Clé InChI

YDBLKRPLXZNVNB-UHFFFAOYSA-N

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.

Actions biochimiques/physiologiques

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.
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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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BPC 157 trifluoroacetate salt ≥95% (HPLC)

Sigma-Aldrich

SML1719

BPC 157 trifluoroacetate salt

Clomiphene citrate salt analytical standard

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C6272

Clomiphene citrate salt

GW6471 ≥98% (HPLC)

Sigma-Aldrich

G5045

GW6471

Bezafibrate ≥98%, solid

Sigma-Aldrich

B7273

Bezafibrate

AICAR ≥98% (HPLC), powder

Sigma-Aldrich

A9978

AICAR

Fenofibrate ≥99%, powder

Sigma-Aldrich

F6020

Fenofibrate

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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