货号 | 17681-1mg |
描述 | Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.1,2 Darglitazone is a TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations by increasing the expression of the p85 subunit of PI3K.3 It increases insulin effectiveness in obese non-insulin-dependent diabetes mellitus subjects.4 Darglitazone promotes adipocyte differentiation by up-regulating the expression of uncoupling protein-2.5 Through PPARγ, darglitazone restores acute inflammatory responses to cerebral hypoxia-ischemia and reduces infarct size in diabetic ob/obmice.6 |
别名 | CP 86,325; |
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.Zhang, B.,Szalkowski, D.,Diaz, E., et al. Potentiation of insulin stimulation of phosphatidylinositol 3-kinase by thiazolidinedione-derived antidiabetic agents in Chinese hamster ovary cells expressing human insulin receptors and L6 myotubes. The Journal of Biological Chemisty 269(41), 25735-25741 (1994). 4.Chaiken, R.L.,Eckert-Norton, M.,Pasmantier, R., et al. Metabolic effects of darglitazone, an insulin sensitizer, in NIDDM subjects. Diabetologia 38, 1307-1312 (1995). 5.Camirand, A.,Marie, V.,Rabelo, R., et al. Thiazolidinediones stimulate uncoupling protein-2 expression in cell lines representing white and brown adipose tissues and skeletal muscle. Endocrinology 139(1), 428-431 (1998). 6.Kumari, R.,Willing, L.B.,Patel, S.D., et al. The PPAR-γ agonist, darglitazone, restores acute inflammatory responses to cerebral hypoxia-ischemia in the diabetic ob/ob mouse. Journal of Cerebral Blood Flow and Metabolism 30(2), 352-360 (2010). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 420.5 |
分子式 | C23H20N2O4S |
CAS号 | 141200-24-0 |
稳定性 | ≥ 2 years |
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