GW501516


Catalog No. size PriceQuantity
M6456-2 2mg solid $98
M6456-10 10mg solid $391

Description

Cas:317318-70-0

Product Information

GW501516 is a PPARδ receptor agonist. Endurobol was entered into clinical development as a drug candidate for metabolic diseases and cardiovascular diseases, and was abandoned in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs.

 

Chemical Formula: C21H18F3NO3S2

 

Exact Mass: 453.068

 

Molecular Weight: 453.4942 

 

Elemental Analysis: C, 55.62; H, 4.00; F, 12.57; N, 3.09; O, 10.58; S, 14.14

 

Synonym: 

 

GW501516

GW-501516

GW 501516

GW1516

GW 1516

GW-1516

GSK-516

GSK 516

GSK516

Endurobol

 

Chemical Name:

{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]-2-methylphenoxy}acetic acid

 

InChi Key:

YDBLKRPLXZNVNB-UHFFFAOYSA-N

 

InChi Code:  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)

 

Smiles Code:

O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)C=C1C

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life:>3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

GW501516 is shown to be the most potent and selective PPARα agonists known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ.

GW501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells.

GW501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.

 

In Vivo

GW501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

 

 

References

 

  1. Chen W, Gao R, Xie X, Zheng Z, Li H, Li S, Dong F, Wang L. A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884. doi: 10.1038/srep09884. PubMed PMID: 25943561; PubMed Central PMCID: PMC4421799.

 

  1. Magliano DC, Penna-de-Carvalho A, Vazquez-Carrera M, Mandarim-de-Lacerda CA, Aguila MB. Short-term administration of GW501516 improves inflammatory state in white adipose tissue and liver damage in high-fructose-fed mice through modulation of the renin-angiotensin system. Endocrine. 2015 Nov;50(2):355-67. doi: 10.1007/s12020-015-0590-1. Epub 2015 Apr 9. PubMed PMID: 25854303.

 

  1. Wang X, Sng MK, Foo S, Chong HC, Lee WL, Tang MB, Ng KW, Luo B, Choong C, Wong MT, Tong BM, Chiba S, Loo SC, Zhu P, Tan NS. Early controlled release of peroxisome proliferator-activated receptor β/δ agonist GW501516 improves diabetic wound healing through redox modulation of wound microenvironment. J Control Release. 2015 Jan 10;197:138-47. doi: 10.1016/j.jconrel.2014.11.001. Epub 2014 Nov 7. PubMed PMID: 25449811.

 

  1. Pokrywka A, Cholbinski P, Kaliszewski P, Kowalczyk K, Konczak D, Zembron-Lacny A. Metabolic modulators of the exercise response: doping control analysis of an agonist of the peroxisome proliferator-activated receptor δ (GW501516) and 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR). J Physiol Pharmacol. 2014 Aug;65(4):469-76. Review. PubMed PMID: 25179079.

 

  1. Mosti MP, Stunes AK, Ericsson M, Pullisaar H, Reseland JE, Shabestari M, Eriksen EF, Syversen U. Effects of the peroxisome proliferator-activated receptor (PPAR)-δ agonist GW501516 on bone and muscle in ovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89. doi: 10.1210/en.2013-1166. Epub 2014 Apr 7. PubMed PMID: 24708238.

 

Products are for research use only. Not for human use.

 

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