| 货号 | 13107-10mg |
| 描述 | Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).1 Presumably through these actions, it blocks the activation of T cells by allogeneic dendritic cells (IC50 = 0.55 nM) without affecting dendritic cells.2,3,4,5 Moreover, pimecrolimus suppresses the generation of pro-inflammatory cytokines by T cells, the release of pre-formed inflammatory mediators from mast cells, and the activation of eosinophils.6,2,7 These effects support the use of pimecrolimus in countering inflammatory skin diseases, such as atopic dermatitis (eczema) and psoriasis.8,9,10 |
| 别名 | Elidel;SDZ-ASM 981; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bochelen, D.,Rudin, M., and Sauter, A. Calcineurin inhibitors FK506 and SDZ ASM 981 alleviate the outcome of focal cerebral ischemic/reperfusion injury. Journal of Pharmacology and Experimental Therapeutics 288(2), 653-659 (1999). 2.Kalthoff, F.S.,Chung, J., and Stuetz, A. Pimecrolimus inhibits up-regulation of OX40 and synthesis of inflammatory cytokines upon secondary T cell activation by allogeneic dendritic cells. Clinical and Experimental Immunology 130, 85-92 (2002). 3.Meingassner, J.G.,Kowalsky, E.,Schwendinger, H., et al. Pimecrolimus does not affect Langerhans cells in murine epidermis. British Journal of Dermatology 149, 853-857 (2003). 4.Kalthoff, F.S.,Chung, J.,Musser, P., et al. Pimecrolimus does not affect the differentiation, maturation and function of human monocyte-derived dendritic cells, in contrast to corticosteroids. Clinical and Experimental Immunology 133, 350-359 (2003). 5.Meingassner, J.G.,Fahrngruber, H., and Bavandi, A. Pimecrolimus inhibits the elicitation phase but does not suppress the sensitization phase in murine contact hypersensitivity, in contrast to tacrolimus and cyclosporine A. Journal of Investigative Dermatology 121(1), 77-80 (2003). 6.Grassberger, M.,Baumruker, T.,Enz, A., et al. A novel anti-inflammatory drug, SDZ ASM 981, for the treatment of skin diseases: In vitro pharmacology. British Journal of Dermatology 141, 264-273 (1999). 7.Plager, D.A.,Henke, S.A.,Matsuwaki, Y., et al. Pimecrolimus reduces eosinophil activation associated with calcium mobilization. International Archives of Allergy and Immunology 149, 119-126 (2009). 8.Rappersberger, K.,Komar, M.,Ebelin, M.E., et al. Pimecrolimus identifies a common genomic anti-inflammatory profile, is clinically highly effective in psoriasis and is well tolerated. Journal of Investigative Dermatology 119(4), 876-887 (2002). 9.Allen, B.R.,Lakhanpaul, M.,Morris, A., et al. Systemic exposure, tolerability, and efficacy of pimecrolimus cream 1% in atopic dermatitis patients. Archives of Disease in Childhood 88, 969-973 (2003). 10.Walling, H.W., and Swick, B.L. Update on the management of chronic eczema: New approaches and emerging treatment options. Clin.Cosmet.Investig.Dermatol. 3, 99-117 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 810.5 |
| 分子式 | C43H68ClNO11 |
| CAS号 | 137071-32-0 |
| 稳定性 | ≥ 2 years |
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