Cilastatin (MK0791)
(Synonyms: 西司他丁; MK0791) 目录号 : GC32162
An inhibitor of dipeptidase (dehydropeptidase I)
Cas No.:82009-34-5
Sample solution is provided at 25 µL, 10mM.
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Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase.1 It inhibits human renal dipeptidase (Ki = 0.7 μM), porcine dipeptidase (IC50 = 0.11 μM), and bacterial metallo-β-lactamase CphA from A. hydrophila (IC50 = 178 μM).1,2,3 Cilastatin (200 μg/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin .4 In a mouse model of systemic infection, cilastatin in combination with imipenem protects mice from S. aureus, E. coli, and P. aeruginosa infection.5 Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life.2 Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections.
1.Campbell, B.J., Forrester, L.J., Zahler, W.L., et al.Beta-lactamase activity of purified and partially characterized human renal dipeptidaseJ. Biol. Chem.259(23)14586-14590(1984) 2.Kahan, F.M., Kropp, H., Sundelof, J.G., et al.Thienamycin: Development of imipenen-cilastatinJ. Antimicrob. Chemother.12(Suppl. D)1-35(1983) 3.Keynan, S., Hooper, N.M., Felici, A., et al.The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-β-lactamase enzyme CphAAntimicrob. Agents Chemother.39(7)1629-1631(1995) 4.Humanes, B., Jado, J.C., Cama?o, S., et al.Protective effects of cilastatin against vancomycin-induced nephrotoxicityBiomed Res. Int.704382(2015) 5.Petersen, P.J., Jacobus, N.V., Weiss, W.J., et al.In vitro and in vivo activities of LJC10,627, a new carbapenem with stability to dehydropeptidase IAntimicrob. Agents Chemother.35(1)203-207(1991)
| Cas No. | 82009-34-5 | SDF | |
| 别名 | 西司他丁; MK0791 | ||
| Canonical SMILES | O=C(O)/C(NC([C@@H]1C(C)(C)C1)=O)=C/CCCCSC[C@H](N)C(O)=O | ||
| 分子式 | C16H26N2O5S | 分子量 | 358.45 |
| 溶解度 | DMSO : 15 mg/mL (41.85 mM) | 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 | 2.7898 mL | 13.9489 mL | 27.8979 mL |
| 5 mM | 0.558 mL | 2.7898 mL | 5.5796 mL |
| 10 mM | 0.279 mL | 1.3949 mL | 2.7898 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