Vaborbactam
(Synonyms: 法硼巴坦,RPX7009) 目录号 : GC19369
Vaborbactam（RPX7009）是一种广谱β-内酰胺酶抑制剂，对KPC、CTX-M、SHV和CMY酶具有特别强效的活性。
Cas No.:1360457-46-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Animal experiment [1]: | |
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Animal models |
Female Swiss Webster mice |
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Preparation Method |
A 24-hour thigh infection model was established using Klebsiella pneumoniae KP1094. After infection, mice were treated with 100 or 300 mg/kg meropenem intraperitoneally every 2 hours for 24 hours alone or in combination with Vaborbactam ranging from 6.25 to 100 mg/kg every 2 hours for 24 hours. |
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Dosage form |
6.25 to 100mg/kg; i.p. |
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Applications |
The addition of Vaborbactam to both meropenem regimens produced bacterial killing in a dose-dependent fashion, with a maximum of bacterial killing of 2.50 log CFU/thigh. |
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References: [1]Sabet M, Tarazi Z, Nolan T, et al. Activity of meropenem-vaborbactam in mouse models of infection due to KPC-producing carbapenem-resistant Enterobacteriaceae[J]. Antimicrobial Agents and Chemotherapy, 2018, 62(1): 10.1128/aac. 01446-17. |
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Vaborbactam (RPX7009) is a broad-spectrum β-lactamase inhibitor with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes[1]. Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase competitive inhibitor used to treat complicated urinary tract infections[2]. Vaborbactam forms a reversible coordination bond with β-lactamases and is not hydrolyzed by β-lactamases[3]. Vaborbactam can enhance the activity of β-lactams against Mycobacterium abscessus[4]. Vaborbactam is often used in combination with Meropenem and has potent in vitro activity against resistant Gram-negative pathogens, especially Klebsiella pneumoniae that produces Klebsiella pneumoniae carbapenemase (KPC), with MIC50 values typically ≤ 0.06µg/ml[5].
In vivo, vaborbactam (6.25-100mg/kg) was injected intraperitoneally in mice to treat a 24-hour thigh infection model of Klebsiella pneumoniae KP1094. Combining it with two meropenem regimens (100 and 300mg/kg) produced a dose-dependent bactericidal effect, with a maximum bactericidal effect of 2.50 log CFU/thigh[6].
References:
[1] Hamrick J C, Docquier J D, Uehara T, et al. VNRX-5133 (taniborbactam), a broad-spectrum inhibitor of serine-and metallo-β-lactamases, restores activity of cefepime in Enterobacterales and Pseudomonas aeruginosa[J]. Antimicrobial Agents and Chemotherapy, 2020, 64(3): 10.1128/aac. 01963-19.
[2] Iqbal Z, Sun J, Yang H, et al. Recent developments to cope the antibacterial resistance via β-lactamase inhibition[J]. Molecules, 2022, 27(12): 3832.
[3] Bookser B C, Reddy K R, Boyer S H, et al. Vaborbactam (in Combination with Meropenem as Vabomere), a Non‐β‐Lactam β‐Lactamase Inhibitor for Treatment of Complicated Urinary Tract Infections and Pyelonephritis[J]. Current Drug Synthesis, 2022: 17-40.
[4] Sanchez L, Bitar M, Herail Q, et al. In vitro and intracellular activity of vaborbactam combined with β-lactams against Mycobacterium abscessus[J]. Journal of Antimicrobial Chemotherapy, 2024, 79(8): 1914-1918.
[5] Wenzler E, Scoble P J. An appraisal of the pharmacokinetic and pharmacodynamic properties of meropenem-vaborbactam[J]. Infectious Diseases and Therapy, 2020, 9(4): 769-784.
[6] Sabet M, Tarazi Z, Nolan T, et al. Activity of meropenem-vaborbactam in mouse models of infection due to KPC-producing carbapenem-resistant Enterobacteriaceae[J]. Antimicrobial Agents and Chemotherapy, 2018, 62(1): 10.1128/aac. 01446-17.
Vaborbactam（RPX7009）是一种广谱β-内酰胺酶抑制剂，对KPC、CTX-M、SHV和CMY酶具有特别强效的活性[1]。Vaborbactam是一种环状硼酸药效团β-内酰胺酶竞争性抑制剂，用于治疗复杂的尿路感染[2]。Vaborbactam通过与β-内酰胺酶形成可逆配价键，不会被β-内酰胺酶水解[3]。Vaborbactam可以提高β-内酰胺对抗脓肿分枝杆菌的活性[4]。Vaborbactam通常与Meropenem联合使用，对耐药革兰氏阴性病原体，特别是产生肺炎克雷伯菌碳青霉烯酶（KPC）的肺炎克雷伯菌具有有效的体外活性，MIC50值通常≤ 0.06µg/ml[5]。
在体内，Vaborbactam（6.25-100mg/kg）通过腹腔注射治疗肺炎克雷伯菌 KP1094建立的24小时大腿感染模型小鼠，联合两种美罗培南方案（100和300 mg/kg）均可产生剂量依赖性杀菌效果，最大杀菌效果为2.50 log CFU/大腿[6]。
| 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 | |||
 |
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。