Avibactam sodium hydrate
(Synonyms: 阿维巴坦钠水合物; NXL-104 hydrate) 目录号 : GC35438
Avibactam (AVE-1330A, NXL104) is a covalent, reversible, non-β-lactam β-lactamase inhibitor with IC50 values of 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively.
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cells (~109 cfu) from overnight broth culture are spread on Mueller-Hinton agar supplemented with either (i) Ceftaroline plus Avibactam (1 or 4 mg/L) at 1-16× the MICs or (ii) Ceftaroline at 1 or 4 mg/L plus Avibactam at 1-8× the concentration needed to reduce the Ceftaroline MIC to 1 or 4 mg/L. Colonies are counted after overnight incubation and representatives are retained[2]. |
Animal experiment: | Mice[3]Avibactam is reconstituted in sterile water to a stock solution of 5,120 mg/L and further solution is prepared in Mueller-Hinton broth. Outbred female CD-1 mice, 7 to 8 weeks old and weighing 20 to 25 g, are used in the experiments. Eight dose combinations are used. For the thigh-infected animals, the combinations of GR20263 and Avibactam are 16/4, 8/1, 64/32, and 2/128 mg/kg. For the lung-infected mice, combinations of 32/16, 4/2, 128/8, and 1/64 mg/kg of the respective constituents are used. These combinations are chosen in order to detect possible pharmacokinetic interactions between the two compounds (GR20263 and Avibactam) and to cover a wide range of doses of each compound. |
References: [1]. Ehmann DE, et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. | |
Avibactam (AVE-1330A, NXL104) is a covalent, reversible, non-β-lactam β-lactamase inhibitor with IC50 values of 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively.
Avibactam (formerly NXL104, AVE1330A) is a synthetic non-β-lactam, β-lactamase inhibitor inhibits the activities of Ambler class A and C β-lactamases and some Ambler class D enzymes[1]. Avibactam has an unusual mechanism of action: it is a covalent inhibitor that acts via ring opening, but in contrast to other currently used β-lactamase inhibitors, this reaction is reversible[2].
[1] Zhanel GG, et al. Drugs. 2013, 73(2):159-77. [2] Lahiri SD, et al. Antimicrob Agents Chemother. 2014, 58(10):5704-13.
| Cas No. | SDF | ||
| 别名 | 阿维巴坦钠水合物; NXL-104 hydrate | ||
| Canonical SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)([O-])=O.O.[Na+] | ||
| 分子式 | C7H12N3NaO7S | 分子量 | 305.24 |
| 溶解度 | Water: ≥ 200 mg/mL (655.22 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。 |
||
| 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 | 3.2761 mL | 16.3806 mL | 32.7611 mL |
| 5 mM | 0.6552 mL | 3.2761 mL | 6.5522 mL |
| 10 mM | 0.3276 mL | 1.6381 mL | 3.2761 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。