产品描述 Pimecrolimus是一种抑免蛋白配体, 可以特异地与胞质受体macrophilin-12结合；是钙调蛋白抑制剂。 靶点（IC50 & Targe） Others, 体外研究 Pimecrolimus通过抑制磷酸酶功能阻断T淋巴细胞激活途径。[1] Pimecrolimus阻止细胞因子和促炎性介质从肥大细胞中释放。Pimecrolimus与macrophilin-12结合，形成pimecrolimus-macrophilin复合物，然后与胞质酶钙调磷酸酶结合。Pimecrolimus-macrophilin复合物通过抑制钙调磷酸酶的作用，阻止活化的T细胞中核因子的细胞质成分去磷酸化。Pimecrolimus不仅抑制肥大细胞中细胞因子的转录和合成，也会通过抑制Fc∈-RI介导的脱粒和分泌而抑制预成形的介质5-羟色胺和β-氨基己糖苷酶的释放。Pimecrolimus治疗引起与macrolactam靶点通路和炎症相关基因的mRNA表达的强烈下调。[2] 体内研究 在小鼠体内，Pimecrolimus口服后与环孢霉素A一样有效，皮下注射后比环孢霉素A略有效。在过敏性接触皮炎小鼠体内，与环孢霉素A和他克莫司相比，Pimecrolimus不间断地抑制次级炎症反应，但是不损害初次免疫反应。[2] 在过敏性接触皮炎(ACD)猪模型中，Pimecrolimus与强效皮质类固醇氯倍他索-17-丙酸盐同样有效。在低镁无毛大鼠，一个模拟急性过敏性皮炎信号的模型中，Pimecrolimus也能有效降低皮肤炎症和瘙痒。在 (1)局部移植物抗宿主反应，(2)用绵羊红细胞形成抗体，和(3)肾移植的大鼠体内，与他克莫司相比，Pimecrolimus仅显示出低电势以减弱全身免疫应答反应。[3] 激酶实验 细胞实验 Cell lines: melanocytes Concentrations: 1, 10, 100, 1,000 nM Incubation Time: 3 days Method: The proliferation rate of melanocytes was determined using a colorimetric MTT assay. Melanocytes were plated in 96-well microplates, and each well was pretreated with 100 µl of different concentrations (1, 10, 100, 1,000 nM) of pimecrolimus for 3 days. Then, 50 µL of 5 mg/mL 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) solution was added to each well. The resulting formazan was dissolved with 150 µL dimethylsulfoxide. The absorbance of the samples was measured at a wavelength of 490 nm. (Only for Reference) 动物实验 参考文献 [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. [4] Xu P, et al. Korean J Physiol Pharmacol. 2017, 21(3):287-292.