For research use only. Not for therapeutic Use.
GW9662 (Cat No.: I002751) is a highly selective antagonist for the Peroxisome Proliferator-Activated Receptor Gamma (PPARγ), with remarkable potency, as evidenced by its IC50 of 3.3 nM in cell-free assays. It exhibits exceptional functional selectivity, being 10 to 600 times more specific for PPARγ compared to PPARα and PPARδ in cellular contexts. At a concentration of 10 μM, GW9662 effectively inhibits the differentiation of adipocytes induced by hormones and agonists, making it a valuable tool for research in areas such as adipocyte biology and metabolic disorders. Its selectivity for PPARγ highlights its importance in studying this receptor’s functions.
| Catalog Number | I002751 |
| CAS Number | 22978-25-2 |
| Synonyms | 2-chloro-5-nitro-N-phenylbenzamide |
| Molecular Formula | C₁₃H₉ClN₂O₃ |
| Purity | ≥95% |
| Target | PPAR |
| Solubility | DMSO 25 mg/ml Ethanol 25 mg/ml |
| Storage | 2-8°C |
| IC50 | 3.3 nM(for PPARγ); 32 nM(for PPARα); 2 uM(for PPARδ) |
| IUPAC Name | 2-chloro-5-nitro-N-phenylbenzamide |
| InChI | InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17) |
| InChIKey | DNTSIBUQMRRYIU-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl |
| Reference | </br>1:BZ-26, a novel GW9662 derivate, attenuated inflammation by inhibiting the differentiation and activation of inflammatory macrophages. Bei Y, Chen J, Zhou F, Huang Y, Jiang N, Tan R, Shen P.Biomed Pharmacother. 2016 Dec;84:730-739. doi: 10.1016/j.biopha.2016.08.069. Epub 2016 Oct 3. PMID: 27710897 </br>2:The PPAR-γ antagonist GW9662 elicits differentiation of M2c-like cells and upregulation of the MerTK/Gas6 axis: a key role for PPAR-γ in human macrophage polarization. Zizzo G, Cohen PL.J Inflamm (Lond). 2015 May 3;12:36. doi: 10.1186/s12950-015-0081-4. eCollection 2015. PMID: 25972766 Free PMC Article</br>3:Limited Applicability of GW9662 to Elucidate PPARγ-Mediated Fatty Acid Effects in Primary Human T-Helper Cells. Jaudszus A, Lorkowski S, Gruen M, Roth A, Jahreis G.Int J Inflam. 2014;2014:149628. doi: 10.1155/2014/149628. Epub 2014 Jun 25. PMID: 25054074 Free PMC Article</br>4:PPAR-γ agonist GW1929 but not antagonist GW9662 reduces TBBPA-induced neurotoxicity in primary neocortical cells. Wojtowicz AK, Szychowski KA, Kajta M.Neurotox Res. 2014 Apr;25(3):311-22. doi: 10.1007/s12640-013-9434-z. Epub 2013 Oct 17. PMID: 24132472 Free PMC Article</br>5:PPARγ antagonist GW9662 induces functional estrogen receptor in mouse mammary organ culture: potential translational significance. Mehta RG, Peng X, Roy S, Hawthorne M, Kalra A, Alimirah F, Mehta RR, Kopelovich L.Mol Cell Biochem. 2013 Jan;372(1-2):249-56. doi: 10.1007/s11010-012-1466-9. Epub 2012 Sep 24. PMID: 23001870 </br>6:Peroxisome proliferator-activated receptor-gamma antagonists GW9662 and T0070907 reduce the protective effects of lipopolysaccharide preconditioning against organ failure caused by endotoxemia. Collin M, Murch O, Thiemermann C.Crit Care Med. 2006 Apr;34(4):1131-8. PMID: 16484917 </br>7:The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Collino M, Patel NS, Lawrence KM, Collin M, Latchman DS, Yaqoob MM, Thiemermann C.Kidney Int. 2005 Aug;68(2):529-36. PMID: 16014029 Free Article</br>8:GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Seargent JM, Yates EA, Gill JH.Br J Pharmacol. 2004 Dec;143(8):933-7. Epub 2004 Nov 8. PMID: 15533890 Free PMC Article</br>9:Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Leesnitzer LM, Parks DJ, Bledsoe RK, Cobb JE, Collins JL, Consler TG, Davis RG, Hull-Ryde EA, Lenhard JM, Patel L, Plunket KD, Shenk JL, Stimmel JB, Therapontos C, Willson TM, Blanchard SG.Biochemistry. 2002 May 28;41(21):6640-50. PMID: 12022867 |
