| 货号 | 10026-1mg |
| 描述 | The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo.1,2 There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.3,4 However, only a few antagonists have been reported.5 T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Willson, T.M.,Cobb, J.E.,Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J. Med. Chem. 39, 665-668 (1996). 2.Cantello, B.C.C.,Cawthorne, M.A.,Cottam, G.P., et al. [[ω-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents. J. Med. Chem. 37, 3977-3985 (1994). 3.Davies, S.S.,Pontsler, A.V.,Marathe, G.K., et al. Oxidized alkyl phospholipids are specific, high affinity peroxisome proliferator-activated receptor γ ligands and agonists. The Journal of Biological Chemisty 276, 16015-16023 (2001). 4.Maxey, K.M.,Hessler, E.,MacDonald, J., et al. The nature and composition of 15-deoxy-Δ12,14-PGJ2. Prostaglandins & Other Lipid Mediators 62, 15-21 (2000). 5.Wright, H.M.,Clish, C.B.,Mikami, T., et al. A synthetic antagonist for the peroxisome proliferator-activated receptor γ inhibits adipocyte differentiation. The Journal of Biological Chemisty 275, 1873-1877 (2000). 6.Lee, G.,Elwood, F.,McNally, J., et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor γ, functions as an antagonist of biochemical and cellular activities. The Journal of Biological Chemisty 277(22), 19649-19657 (2002). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 277.7 |
| 分子式 | C12H8ClN3O3 |
| CAS号 | 313516-66-4 |
| 稳定性 | ≥ 1 year |
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