| 货号 | 10011565-1mg |
| 描述 | Prostaglandin E2(PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).1 L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.2 L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats2 and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.3 At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Coleman, R.A.,Smith, W.L. and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacological Reviews 46, 205-229 (1994). 2.Machwate, M.,Harada, S.,Leu, C.T., et al. Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Molecular Pharmacology 60(1), 36-41 (2001). 3.Takayama, K.,García-Gardeña, G.,Sukhova, G.K., et al. Prostaglandin E2 suppresses chemokine production in human macrophages through the EP4 receptor. The Journal of Biological Chemisty 277(46), 44147-44154 (2002). 4.Cherukuri, D.P.,Chen, X.B.O.,Goulet, A.C., et al. The EP4 receptor antagonist, L-161,982, blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells. Experimental Cell Research 313, 2969-2979 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 654.2 |
| 分子式 | C32H29F3N4O4S2 |
| CAS号 | 147776-06-5 |
| 稳定性 | ≥ 2 years |
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