Avibactam sodium/NXL-104；阿维巴坦钠
货号：
IA1560
品牌：
Jinpan
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产品简介
| 别名 | NXL-104;AVE-1330A |
| 英文名称 | Avibactam sodium/NXL-104 |
| CAS | 1192491-61-4 |
| 分子式 | C7H10N3NaO6S |
| 分子量 | 287.23 |
| 纯度 | HPLC≥98% |
| 单位 | 瓶 |
| 生物活性 | 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 is a novel non-β-lactam β-lactamase inhibitor that inhibits a wide range of β-lactamases. [1-2] |
| In Vitro | 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]. |
| 激酶实验 | The addition of avibactam greatly (4-1024-fold minimum inhibitory concentration [MIC] reduction) improves the activity of ceftazidime versus most species of Enterobacteriaceae depending on the presence or absence of β-lactamase enzyme(s). Against Pseudomonas aeruginosa, the addition of avibactam also improves the activity of ceftazidime (~fourfold MIC reduction). Limited data suggest that the addition of avibactam does not improve the activity of ceftazidime versus Acinetobacter species or most anaerobic bacteria (exceptions: Bacteroides fragilis, Clostridium perfringens, Prevotella spp. and Porphyromonas spp.). The pharmacokinetics of avibactam follow a two-compartment model and do not appear to be altered by the co-administration of ceftazidime. The maximum plasma drug concentration (C(max)) and area under the plasma concentration-time curve (AUC) of avibactam increase linearly with doses ranging from 50 mg to 2,000 mg. The mean volume of distribution and half-life of 22 L (~0.3 L/kg) and ~2 hours, respectively, are similar to ceftazidime.[1] |
| SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)([O-])=O.[Na+] |
| 靶点 | Bacterial |
| 数据来源文献 | [1] Zhanel GG, et al. Drugs. 2013, 73(2):159-77. [2] Lahiri SD, et al. Antimicrob Agents Chemother. 2014, 58(10):5 |
| 规格 | 5mg 10mg 20mg |
是一种可逆的β-内酰胺酶 (β-lactamase) 抑制剂