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Avibactam sodium

产品编号 T4201 CAS 1192491-61-4

别名: 阿维巴坦, AVE-1330A, 阿维巴坦钠, NXL-104

Avibactam sodium (NXL-104) 是一种可逆的 β-内酰胺酶抑制剂，抑制 TEM-1，P99和KPC-2 β-内酰胺酶，IC50分别为8、80和38 nM。

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Avibactam sodium, CAS 1192491-61-4

规格	价格/CNY	货期
2 mg	￥ 279	现货
5 mg	￥ 453	现货
10 mg	￥ 659	现货
25 mg	￥ 1,150	现货
50 mg	￥ 1,860	现货
100 mg	￥ 2,920	现货
200 mg	￥ 4,230	现货
500 mg	￥ 6,590	现货
1 mL * 10 mM (in DMSO)	￥ 578	现货

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其他形式的 Avibactam sodium:

选择批次

纯度: 100%

COA DATASHEET SDS HNMR LCMS

纯度: 99.95%

COA DATASHEET SDS HNMR HPLC

纯度: 99.56%

COA DATASHEET SDS HPLC HNMR

纯度: 99.16%

COA DATASHEET SDS HPLC HNMR

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8/80/38 nM, for TEM-1/P99/KPC-2 β-lactamases).
靶点活性	TEM1:8 nM, P99:80 nM, KPC2:38 nM
体外活性	Avibactam (NXL104) sodium has little antibacterial activity and inhibits class A and C β-lactamases. Except for Metallo types and Acinetobacter OXA carbapenemases, Avibactam inactivates the most of important β-lactamases[2].
体内活性	Avibactam sodium displays a slow return of activity with an off-rate of 0.045±0.022 min-1, which converts to a residence time half-life (tt1/2) of 16±8 min. Avibactam has slow deacylation through hydrolysis or reversibility, and this is in contrast to previously reported extremely long t1/2 values of >1 or >7 d for Avibactam inhibition of TEM-1[1]. Mice are infected with ca.106 CFU of Pseudomonas aeruginosa intramuscularly into the thigh or intranasally to cause pneumonia and are given 8 different (single) subcutaneous doses of Ceftazidime and Avibactam in various combined concentrations, ranging from 1 to 128 mg/kg of body weight in 2-fold increases. The mean estimated half-life in plasma of Ceftazidime in the terminal phase is 0.28 h (SD, 0.02 h), and that of Avibactam is 0.24 h (SD, 0.04 h). Volumes of distribution are 0.80 L/kg (SD, 0.14 L/kg) and 1.18 liters/kg (SD, 0.34 L/kg), respectively.
激酶实验	In a 200 μL reaction volume, 1 μM TEM-1 is incubated with and without 5 μM Avibactam for 5 min at 37°C and subjected to two ultrafiltration cartridge (UFC) steps to remove excess inhibitor (Ultrafree-0.5 with Biomax membrane, 5-kDa cutoff). Centrifugation at 10,600× g for 8 min is performed at 4°C. After each ultrafiltration step, 20 μL retentate is diluted with 180 μL assay buffer to restore the original enzyme concentration. After two UFC treatments, the amount of free Avibactam is quantified by LC/MS/MS and found to be <5% of the original concentration. Loss of protein during UFC is assessed by measuring TEM-1 activity (on 4,000-fold dilution) in the acyl-enzyme sample compare with a non-UFC-treated enzyme, and loss is found to be <5%[1].
细胞实验	Avibactam is prepared in sterile water[2].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].
动物实验	Avibactam is reconstituted in sterile water to a stock solution of 5,120 mg/L and the 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 Ceftazidime 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 (Ceftazidime and Avibactam) and to cover a wide range of doses of each compound.

别名	阿维巴坦, AVE-1330A, 阿维巴坦钠, NXL-104
分子量	287.22
分子式	C7H10N3NaO6S
CAS No.	1192491-61-4

存储

keep away from direct sunlight　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 53 mg/mL (184.5 mM)

H2O: 52 mg/mL (181 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	3.4817 mL	17.4083 mL	34.8165 mL	87.0413 mL
	5 mM	0.6963 mL	3.4817 mL	6.9633 mL	17.4083 mL
	10 mM	0.3482 mL	1.7408 mL	3.4817 mL	8.7041 mL
	20 mM	0.1741 mL	0.8704 mL	1.7408 mL	4.3521 mL
	50 mM	0.0696 mL	0.3482 mL	0.6963 mL	1.7408 mL
	100 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8704 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

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. 2. Livermore DM, et al. Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104). J Antimicrob Chemother. 2012 Jun;67(6):1354-8. 3. Berkhout J, et al. Pharmacokinetics and penetration of ceftazidime and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Avibactam sodium 1192491-61-4 Microbiology/Virology Antibacterial Antibiotic 阿维巴坦 inhibit antibacterial Avibactam AVE-1330A NXL 104 Bacterial TEM-1 β-lactamase Inhibitor Klebsiella pneumonia Pseudomonas aeruginosa 阿维巴坦钠 NXL-104 NXL104 inhibitor

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Avibactam sodium

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords