SML1491
GW501516
≥98% (HPLC)
동의어(들):
2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-acetic acid, GW1516
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C21H18F3NO3S2
CAS Number:
Molecular Weight:
453.50
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77
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추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 20 mg/mL, clear
저장 온도
−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
애플리케이션
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[1]
- in organoid culture medium to test its effect on self-renewal of PR domain containing 16 (Prdm16)-depleted intestinal stem cells[2]
- as a component in the defatting medium for primary human hepatocytes (PHH) culture[3]
GW501516 has been used to study its effect on mutation-driven colorectal tumorigenesis and tumor invasion using mouse model.[4]
생화학적/생리학적 작용
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.[5] 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.[6]
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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시험 성적서(COA)
Lot/Batch Number
이미 열람한 고객
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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