Date published: 2025-12-18

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GW501516 (CAS 317318-70-0)

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Alternate Names:
2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid; Endurobol
Application:
GW501516 is a selective and potent PPARβ agonist
CAS Number:
317318-70-0
Purity:
≥97%
Molecular Weight:
453.50
Molecular Formula:
C21H18F3NO3S2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GW501516 is the most selective and potent PPARbeta (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes. Studies demonstrate that GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, GW501516 may act to block insulin resistance and fatty acid-induced nuclear factor-kappaB (NF-κB) activation.


GW501516 (CAS 317318-70-0) References

  1. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.  |  Oliver, WR., et al. 2001. Proc Natl Acad Sci U S A. 98: 5306-11. PMID: 11309497
  2. Peroxisome proliferator-activated receptor (PPAR) alpha and PPARbeta/delta, but not PPARgamma, modulate the expression of genes involved in cardiac lipid metabolism.  |  Gilde, AJ., et al. 2003. Circ Res. 92: 518-24. PMID: 12600885
  3. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.  |  Sznaidman, ML., et al. 2003. Bioorg Med Chem Lett. 13: 1517-21. PMID: 12699745
  4. The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells.  |  Dressel, U., et al. 2003. Mol Endocrinol. 17: 2477-93. PMID: 14525954
  5. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta.  |  Wei, ZL. and Kozikowski, AP. 2003. J Org Chem. 68: 9116-8. PMID: 14604391
  6. Synthesis of the PPARbeta/delta-selective agonist GW501516 and C4-thiazole-substituted analogs.  |  Pereira, R., et al. 2006. Bioorg Med Chem Lett. 16: 49-54. PMID: 16242326
  7. Effects of bezafibrate, PPAR pan-agonist, and GW501516, PPARdelta agonist, on development of steatohepatitis in mice fed a methionine- and choline-deficient diet.  |  Nagasawa, T., et al. 2006. Eur J Pharmacol. 536: 182-91. PMID: 16574099
  8. The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells.  |  Dimopoulos, N., et al. 2007. FEBS Lett. 581: 4743-8. PMID: 17869249
  9. Activation of peroxisome proliferator-activated receptor-{delta} by GW501516 prevents fatty acid-induced nuclear factor-{kappa}B activation and insulin resistance in skeletal muscle cells.  |  Coll, T., et al. 2010. Endocrinology. 151: 1560-9. PMID: 20185762
  10. The peroxisome proliferator-activated receptor β/Δ (PPARβ/Δ) agonist GW501516 prevents TNF-α-induced NF-κB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1.  |  Barroso, E., et al. 2011. Biochem Pharmacol. 81: 534-43. PMID: 21146504
  11. GW501516, a PPARΔ agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFκB pathway in mice.  |  Yang, X., et al. 2011. PLoS One. 6: e25271. PMID: 21966476
  12. The peroxisome proliferator-activated receptor (PPAR) β/Δ agonist GW501516 inhibits IL-6-induced signal transducer and activator of transcription 3 (STAT3) activation and insulin resistance in human liver cells.  |  Serrano-Marco, L., et al. 2012. Diabetologia. 55: 743-51. PMID: 22179221
  13. GW501516-activated PPARβ/Δ promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation.  |  Kostadinova, R., et al. 2012. Cell Biosci. 2: 34. PMID: 23046570
  14. 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.  |  Magliano, DC., et al. 2015. Endocrine. 50: 355-67. PMID: 25854303
  15. A metabolomic study of the PPARΔ agonist GW501516 for enhancing running endurance in Kunming mice.  |  Chen, W., et al. 2015. Sci Rep. 5: 9884. PMID: 25943561

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GW501516, 1 mg

sc-202642
1 mg
$80.00

GW501516, 5 mg

sc-202642A
5 mg
$175.00

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. This chemical is supplied as a white powder. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2021-07-15
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Rated 5 out of 5 by from Amazing stuffLet's just say this stuff is my little secret *wink wink*
Date published: 2022-07-14
Rated 5 out of 5 by from we use it all the timewe use it all the time, order only from you, works well, very consistent
Date published: 2015-04-07
Rated 5 out of 5 by from Kim et alKim et al. (PubMed ID 19461048) used GW501516, a PPAR agonist, to enhance the expression of extracellular matrix proteins necessary to maintain sturdiness of atherosclerotic plaques. -SCBT Publication Review
Date published: 2015-04-07
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GW501516 is rated 5.0 out of 5 by 3.
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