| Description | Pimecrolimus (SDZ-ASM 981), a calcineurin inhibitor immunosuppressant, binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. |
| In vitro | Pimecrolimus在多种过敏性动物中能够有效改善过敏症状.在模拟急性过敏性皮炎低镁无毛大鼠模型和中过敏性接触皮炎小鼠中,Pimecrolimus抑制炎症反应和瘙痒症状. |
| In vivo | 肥大细胞中,Pimecrolimus阻止细胞因子的转录和合成,同时促进5-羟色胺和β-氨基己糖苷酶的释放。在T淋巴细胞中,Pimecrolimus通过抑制磷酸酶功能,阻断T细胞激活。 |
| Synonyms | SDZ-ASM 981, ASM 981, 吡美莫司 |
| molecular weight | 810.45 |
| Molecular formula | C43H68ClNO11 |
| CAS | 137071-32-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 93 mg/mL (114.8 mM) DMSO: 93 mg/mL (114.8 mM) |
| References | 1. Nghiem P, et al. Am Acad Dermatol, 2002, 46(2), 228-241. 2. Gupta AK, et al. J Eur Acad Dermatol Venereol, 2003, 17(5), 493-503. 3. Stuetz A, et al. Semin Cutan Med Surg, 2001, 20(4), 233-241. |