货号 | 71000-1ea |
描述 | The Cayman PPARγ Ligand Pack contains a combination of frequently used ligands for the nuclear PPARγ. Each kit contains Ciglitazone, the first characterized member of the thiazolidinedione (TZD) class that binds to the PPARγ ligand-binding domain with an EC50 value of 3.0 µM.1,2 Rosiglitazone, a key reference TZD also called BRL 49653, its more potent structural homolog MCC-555, and PPARγ-1-selective pioglitazone are other PPARγ agonists provided. Also included is Troglitazone (Resulin™), another TZD; it was withdrawn from human therapeutic use due to hepatotoxicity.3 Also in this assortment is 15-deoxy-Δ12,14-Prostaglandin J2, a potent PPARγ ligand derived from PGD2. The actions of all of these compounds can be antagonized by the selective PPARγ antagonist, GW 9662, which is also in the kit.4 |
别名 | Peroxisome Proliferator-activated Receptor γ Pack; |
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.Sohda, T.,Mizuno, K.,Imaniya, E., et al. Studies on antidiabetic agents. II. Synthesis of 5-[4-(1-methylcyclohexylmethoxy)-benzyl]thiazolidine-2,4-dione (ADD-3878) and its derivatives. Chemical & Pharmaceutical Bulletin 30(10), 3580-3600 (1982). 3.Kodera, Y.,Takeyama, K.i.,Murayama, A., et al. Ligand type-specific interactions of peroxisome proliferator-activated receptor γ with transcriptional coactivators. The Journal of Biological Chemisty 275, 33201-33204 (2000). 4.Bendixen, A.C.,Shevde, N.K.,Dienger, K.M., et al. IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1. Proceedings of the National Academy of Sciences of the United States of America 98, 2443-2448 (2001). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | >98% |
稳定性 | ≥ 1 year |
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