Pimecrolimus
(Synonyms: 吡美莫司; SDZ-ASM 981) 目录号 : GC10825
Anti-inflammatory macrolactam
Cas No.:137071-32-0
Sample solution is provided at 25 µL, 10mM.
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Pimecrolimus is a cell-selective inhibitor of inflammatory cytokines secretion in T cells and mast cells [1].
Inflammatory cytokines are cytokines which promote systemic inflammation. Pimecrolimus can be used for the treatment of inflammatory skin diseases, such as plaque-type psoriasis, atopic dermatitis, irritant contact dermatitis and allergic contact dermatitis [1].
Pimecrolimus is a cell-selective inflammatory cytokines secretion inhibitor. Pimecrolimus inhibited the secretion of inflammatory cytokines in mast cells and T cells and also inhibited the release of preformed inflammatory mediators from mast cells. Pimecrolimus exhibited a low potential to impair systemic immune reactions in the skin [1]. In peripheral blood leukocytes contained basophil or mast cells, pimecrolimus inhibited histamine release induced by anti-IgE from basophils and mast cells by 82% and 73%, respectively. Also, pimecrolimus inhibited tryptase, LTC4 and TNF-alpha release [2]. In CD4+ T cells stimulated by dendritic cells (DC), pimecrolimus inhibited the up-regulation of CD25 and CD54 and surface expression of OX40. Pimecrolimus inhibited T cell proliferation with IC50 value of 0.55 nM and inhibited the synthesis of IFN-γ and TNF-α [3].
In treatment of allergic contact dermatitis (ACD) mice and rats, pimecrolimus exhibited a higher potency. In atopic dermatitis rats, pimecrolimus effectively reduced pruritus and skin inflammation [1].
References:
[1]. Stuetz A, Grassberger M, Meingassner JG. Pimecrolimus (Elidel, SDZ ASM 981)--preclinical pharmacologic profile and skin selectivity. Semin Cutan Med Surg, 2001, 20(4): 233-241.
[2]. Zuberbier T, Chong SU, Grunow K, et al. The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils. J Allergy Clin Immunol, 2001, 108(2): 275-280.
[3]. Kalthoff FS, Chung J, Stuetz A. Pimecrolimus inhibits up-regulation of OX40 and synthesis of inflammatory cytokines upon secondary T cell activation by allogeneic dendritic cells. Clin Exp Immunol, 2002, 130(1): 85-92.
| Cas No. | 137071-32-0 | SDF | |
| 别名 | 吡美莫司; SDZ-ASM 981 | ||
| Canonical SMILES | CO[C@@H]1C[C@H](/C=C(C)/[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@H]([C@@H](OC)C[C@H](C/C(C)=C/4)C)[C@@H](OC)C[C@H]3C)=O)=O)=O)[C@H](C)[C@H](CC([C@@H]4CC)=O)O)CC[C@@H]1Cl | ||
| 分子式 | C43H68ClNO11 | 分子量 | 810.45 |
| 溶解度 | ≥ 32.05mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2339 mL | 6.1694 mL | 12.3388 mL |
| 5 mM | 0.2468 mL | 1.2339 mL | 2.4678 mL |
| 10 mM | 0.1234 mL | 0.6169 mL | 1.2339 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet