Relebactam
(Synonyms: 瑞来巴坦,MK-7655) 目录号 : GC19308
A β-lactamase inhibitor
Cas No.:1174018-99-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target: beta-lactamaseImipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 ug/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 ug/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 ug/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 ug/ml.[1] Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.[2]
References:
[1]. Lapuebla A, et al. Activity of Imipenem with Relebactam against Gram-Negative Pathogens from New York City. Antimicrob Agents Chemother. 2015 Aug;59(8):5029-31.
[2]. Bush K. A resurgence of β-lactamase inhibitor combinations effective against multidrug-resistant Gram-negative pathogens. Int J Antimicrob Agents. 2015 Nov;46(5):483-93.
| Cas No. | 1174018-99-5 | SDF | |
| 别名 | 瑞来巴坦,MK-7655 | ||
| Canonical SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(NC3CCNCC3)=O)[N@@](C2)C1=O)(O)=O | ||
| 分子式 | C12H20N4O6S | 分子量 | 348.38 |
| 溶解度 | Water : 72 mg/mL (206.67 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 | 2.8704 mL | 14.3521 mL | 28.7043 mL |
| 5 mM | 0.5741 mL | 2.8704 mL | 5.7409 mL |
| 10 mM | 0.287 mL | 1.4352 mL | 2.8704 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。