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CAS
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1192491-61-4
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中文名称
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阿维巴坦钠
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英文名称
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Avibactam sodium
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别名
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NXL-104;AVE-1330A
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纯度
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HPLC≥98%
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分子式
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C7H10N3NaO6S
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分子量
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287.23
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外观（性状）
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White to off-white Solid
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储存条件
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Powder : -20℃, 2 years;In solvent(母液): -20℃, 1 month; -80℃, 6 months
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溶解性
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Soluble in Water/DMSO
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InChIKey
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RTCIKUMODPANKX-JBUOLDKXSA-M
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InChI
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InChI=1S/C7H11N3O6S.Na/c8-6(11)5-2-1-4-3-9(5)7(12)10(4)16-17(13,14)15;/h4-5H,1-3H2,(H2,8,11)(H,13,14,15);/q;+1/p-1/t4-,5+;/m1./s1
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PubChem CID
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24944097
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SMILES
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O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)([O-])=O.[Na+]
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描述
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Avibactam sodium/NXL-104是一种可逆的β-内酰胺酶 (β-lactamase) 抑制剂(Avibactam sodium/NXL-104 is a reversible β-lactamase inhibitor)
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靶点
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β-lactamase
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通路
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Anti-infection
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生物活性
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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]
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In Vitro
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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].
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激酶实验
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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]
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数据来源文献
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[1] Zhanel GG, et al. Drugs. 2013, 73(2):159-77.
[2] Lahiri SD, et al. Antimicrob Agents Chemother. 2014, 58(10):5
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规格
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5mg 10mg 20mg
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单位
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瓶
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