阿维巴坦钠|T4201|TargetMol

Avibactam sodium
1192491-61-4

￥279 2mg 起订

￥453 5mg 起订

￥659 10mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 阿维巴坦钠

英文名称：: Avibactam sodium

CAS号：: 1192491-61-4

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.95%

产品类别：: 抑制剂

货号：: T4201

Product Introduction

Bioactivity

名称	Avibactam sodium
描述	Avibactam sodium (NXL-104) is a non-β-lactam β-lactamase inhibitor that inhibits TEM-1, P99, and KPC-2 β-lactamases (IC50=8/80/38 nM) covalently and reversibly. Avibactam sodium has antimicrobial activity and can be used to treat urinary tract infections.
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].
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].
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.
体外活性	方法：产 KPC 的肺炎克雷伯菌用 Avibactam sodium (1-64 mg/L) 和 Ceftazidime (0.0625-512 mg/L) 处理，通过 broth microdilution method 测定 MICs。结果：CAZ-AVI 易感菌株和 CAZ-AVI 耐药菌株的 Ceftazidime MIC 值与 Avibactam 浓度的增加几乎呈对数线性下降。[1]
体内活性	方法：为检测体内抗感染活性，将 Avibactam sodium (4-24 mg/kg，每 2 h 到每 12 h) 和 Ceftazidime 皮下注射给绿脓杆菌感染的 CD-1 小鼠。结果：给药 Avibactam q2h 明显更有效，将 Avibactam 静效的日剂量降低了 2.7 和 10.1 倍，而两种方案的给药间隔中游离药物浓度保持在 1 mg/L 阈值浓度以上产生抑菌作用的平均百分比相似，平均值为 21.6 (q2h) 和 18.5 (q8h)。[2]
存储条件	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 16.67 mg/mL (58.03 mM) H2O : 52 mg/mL (181 mM)
关键字	inhibit \| antibacterial \| Avibactam \| Avibactam sodium \| NXL 104 \| Antibiotic \| Bacterial \| TEM-1 \| β-lactamase \| Inhibitor \| Klebsiella pneumonia \| Pseudomonas aeruginosa \| NXL104
相关产品	Crystal Violet \| Dehydroacetic acid sodium \| G-418 disulfate \| Doxycycline \| Methyl anthranilate \| Neomycin sulfate \| Metronidazole \| Dimethyl sulfoxide \| EDTA copper(II) disodium salt \| Ampicillin sodium \| Sulfamethoxazole sodium \| Kanamycin sulfate
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 药物片段库 \| FDA上市及药典收录分子库 \| 高选择性抑制剂库 \| 非甾体类抗炎化合物库 \| NO PAINS 化合物库 \| FDA 上市药物库 \| 药物功能重定位化合物库

阿维巴坦钠|||阿维巴坦|||NXL-104|||AVE-1330A|TargetMol

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