| 货号 | 10028-1mg |
| 描述 | Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo.1,2 Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.3 Pioglitazone is a closely related TZD which also selectively activates PPARγ-1. Pioglitazone is about one tenth as potent as rosiglitazone, with an EC50 of about 500-600 nM for both human and murine PPARγ.4,5 In a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα, pioglitazone and rosiglitazone exhibit low level activation of PPARα at 1 µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10 µM.4 |
| 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.Lehmann, J.M.,Moore, L.B.,Smith-Oliver, T.A., et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ). J. Biol. Chem. 270, 12953-12956 (1995). 4.Sakamoto, J.,Kimura, H.,Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochemical and Biophysical Research Communications 278, 704-711 (2000). 5.Willson, T.M.,Brown, P.J.,Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. Journal of Medicinal Chemistry 43(4), 528-550 (2000). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 394.5 |
| 分子式 | C19H19N2O3S • K |
| CAS号 | 1266523-09-4 |
| 稳定性 | ≥ 1 year |
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