产品说明书
Pimecrolimus
 |
同义名 : | SDZ-ASM 981;Elidel;Rizan;Brand name: Aregen;33-epi-Chloro-33-desoxyascomycin;Pimecrolimusum;ASM-981 |
| CAS号 : | 137071-32-0 | |
| 货号 : | A944531 | |
| 分子式 : | C43H68ClNO11 | |
| 纯度 : | 98% | |
| 分子量 : | 810.453 | |
| MDL号 : | MFCD00901792 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 30 mg/mL(37.02 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Calcineurin, a critical calcium-activated protein phosphatase, is required for many functions in a variety of tissues: learning and memory, renal function, and the immune response. Pimecrolimus, a novel calcineurin inhibitor closely related to tacrolimus, is also being developed for atopic dermatitis therapy[3]. Pimecrolimus selectively inhibited the activation of T cells and mast cells, two key events in the pathogenesis of AD (atopic dermatitis). In rat model of immunosuppression, the graft-versus-host (GvH) reaction is inhibited by pimecrolimus in a dose-dependent fashion after subcutaneous administration with an ID50 (dose inhibiting the swelling observed in controls by 50%) of 20 mg/kg[4]. In the pig model a statistically significant anti-inflammatory effect was observed at concentrations as low as 0.04%. In the allogenic kidney transplantation model, pimecrolimus prevented organ rejection at oral doses of 15.6 mg/kg and higher. Pimecrolimus doses of 20 mg b.i.d and 30 mg b.i.d. were observed to have the greatest reduction in the Psoriasis Area and Severity Index (PASI) of 60% and 75%, respectively, compared to 4% for placebo[5].. | ||
| 作用机制 | The mechanism of action of pimecrolimus is the blockage of T cell activation involving its binding to macrophilin-12[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00377962 | Disorder Related to Cardiac Tr... 展开 >>ansplantation 收起 << | Phase 4 | Completed | - | Denmark ... 展开 >> Novartis Investigative Site Arhus, Denmark, DK-8200 Novartis Investigative Site Copenhagen, Denmark, 2100 Norway Novartis Investigative Site Oslo, Norway Sweden Novartis Investigative Site Goteborg, Sweden, 413 45 Novartis Investigative Site Linkoping, Sweden, 581 85 Novartis Investigative Site Lund, Sweden, 22185 收起 << |
| NCT00377962 | - | Completed | - | - | |
| NCT00148746 | Moderate to Severe Atopic Derm... 展开 >>atitis 收起 << | Not Applicable | Completed | - | Germany ... 展开 >> Department of Dermatology, TU Dresden Dresden, Germany, 01307 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.23mL 0.25mL 0.12mL |
6.17mL 1.23mL 0.62mL |
12.34mL 2.47mL 1.23mL |
