For research use only. Not for therapeutic Use.
GW0742（Cat No.:I003134）is a potent and selective agonist of the peroxisome proliferator-activated receptor delta (PPARδ), a nuclear receptor involved in regulating lipid metabolism, inflammation, and cellular energy homeostasis. It is primarily studied for its potential therapeutic effects in metabolic disorders, cardiovascular diseases, and obesity. By activating PPARδ, GW0742 enhances fatty acid oxidation, reduces lipid accumulation, and may improve insulin sensitivity. Research also suggests its role in promoting endurance exercise capacity and modulating inflammation. GW0742 is still under investigation for its clinical efficacy and safety across various conditions.
| Catalog Number | I003134 |
| CAS Number | 317318-84-6 |
| Synonyms | 2-[4-[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methylsulfanyl]-2-methylphenoxy]acetic acid |
| Molecular Formula | C21H17F4NO3S2 |
| Purity | ≥95% |
| Target | Vitamin D Related/Nuclear Receptor |
| Solubility | DMSO: ≥ 34 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 1nM, 1.1μM and 2 μM (EC50, for PPARδ, -α, and -γ) |
| IUPAC Name | 2-[4-[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methylsulfanyl]-2-methylphenoxy]acetic acid |
| InChI | InChI=1S/C21H17F4NO3S2/c1-11-7-14(4-6-17(11)29-9-19(27)28)30-10-18-12(2)26-20(31-18)13-3-5-15(16(22)8-13)21(23,24)25/h3-8H,9-10H2,1-2H3,(H,27,28) |
| InChIKey | HWVNEWGKWRGSRK-UHFFFAOYSA-N |
| SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC(=C(C=C3)C(F)(F)F)F)C)OCC(=O)O |
| Reference | </br>1:The Non-Genomic Effects of the PPARβγ agonist GW0742 on STZ treated rat aorta. Perez-Diaz N, Pushkarskya I, Oweisa N, Lionea LA, Mackenzie LS.Curr Mol Pharmacol. 2016 Dec 29. [Epub ahead of print] PMID: 28034288 </br>2:Effect of PPAR-β/δ agonist GW0742 treatment in the acute phase response and blood-brain barrier permeability following brain injury. Chehaibi K, le Maire L, Bradoni S, Escola JC, Blanco-Vaca F, Slimane MN.Transl Res. 2017 Apr;182:27-48. doi: 10.1016/j.trsl.2016.10.004. Epub 2016 Oct 18. PMID: 27818230 </br>3:Pulmonary Administration of GW0742, a High-Affinity Peroxisome Proliferator-Activated Receptor Agonist, Repairs Collapsed Alveoli in an Elastase-Induced Mouse Model of Emphysema. Ozawa C, Horiguchi M, Akita T, Oiso Y, Abe K, Motomura T, Yamashita C.Biol Pharm Bull. 2016;39(5):778-85. doi: 10.1248/bpb.b15-00909. PMID: 27150147 Free Article</br>4:PPARδ agonist GW0742 ameliorates Aβ1-42-induced hippocampal neurotoxicity in mice. An YQ, Zhang CT, Du Y, Zhang M, Tang SS, Hu M, Long Y, Sun HB, Hong H.Metab Brain Dis. 2016 Jun;31(3):663-71. doi: 10.1007/s11011-016-9800-7. Epub 2016 Feb 11. PMID: 26864581 </br>5:Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Niu HS, Ku PM, Niu CS, Cheng JT, Lee KS.Drug Des Devel Ther. 2015 Oct 14;9:5625-32. doi: 10.2147/DDDT.S95045. eCollection 2015. PMID: 26508837 Free PMC Article</br>6:The PPARβ/δ Agonist GW0742 Induces Early Neuronal Maturation of Cortical Post-Mitotic Neurons: Role of PPARβ/δ in Neuronal Maturation. Benedetti E, Di Loreto S, D/’Angelo B, Cristiano L, d/’Angelo M, Antonosante A, Fidoamore A, Golini R, Cinque B, Cifone MG, Ippoliti R, Giordano A, Cimini A.J Cell Physiol. 2016 Mar;231(3):597-606. doi: 10.1002/jcp.25103. PMID: 26206209 </br>7:Chronic peroxisome proliferator-activated receptorβ/δ agonist GW0742 prevents hypertension, vascular inflammatory and oxidative status, and endothelial dysfunction in diet-induced obesity. Toral M, Gómez-Guzmán M, Jiménez R, Romero M, Zarzuelo MJ, Utrilla MP, Hermenegildo C, Cogolludo Á, Pérez-Vizcaíno F, Gálvez J, Duarte J.J Hypertens. 2015 Sep;33(9):1831-44. doi: 10.1097/HJH.0000000000000634. PMID: 26147382 </br>8:Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs. Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, Yuan N, Preston J, Goy R, Arnold LA.J Biomol Res Ther. 2014;3(1). pii: 1000111. PMID: 25485183 Free PMC Article</br>9:The peroxisome proliferator-activated receptor β/δ agonist GW0742 has direct protective effects on right heart hypertrophy. Kojonazarov B, Luitel H, Sydykov A, Dahal BK, Paul-Clark MJ, Bonvini S, Reed A, Schermuly RT, Mitchell JA.Pulm Circ. 2013 Dec;3(4):926-35. doi: 10.1086/674755. Erratum in: Pulm Circ. 2014 Jun;4(2):352. PMID: 25006409 Free PMC Article</br>10:The PPARβ/δ agonist GW0742 modulates signaling pathways associated with cardiac myocyte growth via a non-genomic redox mechanism. Galatou E, Kelly T, Lazou A.Mol Cell Biochem. 2014 Oct;395(1-2):145-54. doi: 10.1007/s11010-014-2120-5. Epub 2014 Jun 18. PMID: 24939361 |
