| 货号 | 17413-1mg |
| 描述 | Tenidap is a COX-1 selective non-steroidal anti-inflammatory drug (IC50s = <0.03, 1.2, and >30 µM for COX-1, COX-2, and 5-lipoxygenase (5-LO), respectively).1 It has anti-inflammatory and antirheumatic properties.1,2In vitro, it inhibits prostaglandin D2(PGD2), leukotriene B4(LTB4), and prostaglandin E2(PGE2) synthesis (IC50s = 0.02, 18, and 32 µM, respectively).3,4 Tenidap also reversibly and dose-dependently activates hKir2.3 channels in CHO cells (EC50 = 402 nM) and inhibits fatty acid amide hydrolase (FAAH) activity.5,6 A formulation containing tenidap was not approved for rheumatoid and osteoarthritis by the FDA due to adverse effects, including bone mineralization loss, as well as liver and kidney toxicity. |
| 别名 | CP 66,248; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kirchner, T.,Argentieri, D.C.,Barbone, A.G., et al. Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation. Journal of Pharmacology and Experimental Therapeutics 282, 1094-1101 (1997). 2.Blackburn, W.D., Jr.,Prupas, H.M.,Silverfield, J.C., et al. Tenidap in rheumatoid arthritis. A 24-week double-blind comparison with hydroxychloroquine-plus-piroxicam, and piroxicam alone. Arthritis Rheum. 38(10), 1447-1456 (1995). 3.Moilanen, E.,Alanko, J.,Asmawi, M.Z., et al. CP-66,248, a new anti-inflammatory agent, is a potent inhibitor of leukotriene B4 and prostanoid synthesis in human polymorphonuclear leucocytes in vitro. Eicosanoids 1(1), (1988). 4.Moore, P.F.,Larson, D.L.,Otterness, I.G., et al. Tenidap, a structurally novel drug for the treatment of arthritis: antiinflammatory and analgesic properties. Inflamm. Res. 45(2), 54-61 (1996). 5.Liu, Y.,Liu, D.,Printzenhoff, D., et al. Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3. Eur. J. Pharmacol. 435(2-3), 153-160 (2002). 6.Bertolacci, L.,Romeo, E.,Veronesi, M., et al. A binding site for nonsteroidal anti-inflammatory drugs in fatty acid amide hydrolase. Journal of the American Chemical Society 135(1), 22-25 (2013). | |
| 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 | 320.8 |
| 分子式 | C14H9ClN2O3S |
| CAS号 | 120210-48-2 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |