Vaborbactam (Synonyms: RPX7009)
目录号: PL12278 纯度: ≥99%
CAS No. :1360457-46-0
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中文名称
Vaborbactam
中文别名
Vaborbactam
英文名称
Vaborbactam
英文别名
Vaborbactam;RPX7009;RPX-7009;2-((3R,6S)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid;1C75676F8V;2-[(3R,6S)-2-hydroxy-3-[(2-thiophen-2-ylacetyl)amino]oxaborinan-6-yl]acetic acid;Vaborbactam [INN];RPX 7009;Vaborbactam. RPX7009;Vaborbactam (USAN/INN);Vaborbactam [USAN:INN];GTPL10871;Vabomere (vaborbactam + meropenem);BDBM50089084;DB12107;SB17184;1,2-Oxaborinane-6-acetic acid, 2-hydrox
Cas No.
1360457-46-0
分子式
C12H16BNO5S
分子量
297.14
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Vaborbactam (RPX7009) 是一种环状硼酸药效团 β-内酰胺酶 (β-lactamase) 抑制剂。
生物活性
Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
性状
Solid
体外研究(In Vitro)
Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes. Vaborbactam restores SM 7338 activity for 72.7 to 98.1% of CPE isolates at ≤2 μg/mL, and maximum potentiation is achieved with fixed concentrations of ≥8 μg/mL of the inhibitor (≥96.5% of isolates are inhibited at ≤2 μg/mL of SM 7338-vaborbactam). SM 7338-vaborbactam with a fixed concentration of 8 μg/mL of the inhibitor (MIC50, ≤0.06 μg/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated SM 7338 MICs at ≤1 μg/mL. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Hecker SJ, et al. Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. J Med Chem. 2015 May 14;58(9):3682-92.
[2]. Castanheira M, et al. Effect of the β-Lactamase Inhibitor Vaborbactam Combined with SM 7338 against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8.
溶解度数据
In Vitro: H2O : 5.26 mg/mL (17.70 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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