Vaborbactam
(Synonyms: 法硼巴坦,RPX7009) 目录号 : GC19369
A β-lactamase inhibitor
Cas No.:1360457-46-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes[1]. Vaborbactam restores meropenem activity for 72.7 to 98.1% of CPE isolates at ≤2 ug/mL, and maximum potentiation is achieved with fixed concentrations of ≥8 ug/mL of the inhibitor (≥96.5% of isolates are inhibited at ≤2 ug/mL of meropenem-vaborbactam). Meropenem-vaborbactam with a fixed concentration of 8 ug/mL of the inhibitor (MIC50, ≤0.06 ug/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated meropenem MICs at ≤1 ug/mL[2]. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase[3].
Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects[3].
References:
[1]. Hecker SJ, et al. Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. J Med Chem. 2015 May 14;58(9):3682-92.
[2]. Castanheira M, et al. Effect of the β-Lactamase Inhibitor Vaborbactam Combined with Meropenem against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8.
[3]. Wong D, et al. Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy.
| Cas No. | 1360457-46-0 | SDF | |
| 别名 | 法硼巴坦,RPX7009 | ||
| Canonical SMILES | O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1 | ||
| 分子式 | C12H16BNO5S | 分子量 | 297.14 |
| 溶解度 | Water : 5.26 mg/mL (17.70 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 | 3.3654 mL | 16.8271 mL | 33.6542 mL |
| 5 mM | 0.6731 mL | 3.3654 mL | 6.7308 mL |
| 10 mM | 0.3365 mL | 1.6827 mL | 3.3654 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。