Vaborbactam-RPX7009-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVaborbactamCat. No.: HY-19930CAS No.: 1360457-46-0Synonyms: RPX7009分式: CHBNOS分量: 297.14作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 5.26 mg/mL (17.70 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3654 mL 16.8271 mL 33.6542 mL5 mM 0.6731 mL 3.3654 mL 6.7308 mL10 mM 0.3365 mL 1.6827 mL 3.3654 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)

3、儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 108 mM sodium carbonateSolubility: 25 mg/mL (84.14 mM); Clear solution; Need ultrasonicBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Vaborbactam種環(huán)狀硼酸藥效團(tuán)-內(nèi)酰胺酶抑制劑。體外研究 Vaborbactam is a broad spectrum of inhibition of -lactamas

4、es, with particularly potent activity against KPC,CTX-M, SHV, and CMY enzymes 1. Vaborbactam restores meropenem activity for 72.7 to 98.1% of CPEisolates at 2 g/mL, and maximum potentiation is achieved with fixed concentrations of 8 g/mL of theinhibitor (96.5% of isolates are inhibited at 2 g/mL of

5、meropenem-vaborbactam). Meropenem-vaborbactamwith a fixed concentration of 8 g/mL of the inhibitor (MIC50, 0.06 g/mL for all organisms) inhibits 93.7% ofthe CPE isolates displaying elevated meropenem MICs at 1 g/mL 2. By forming a reversible dative bondwith the blactamase, vaborbactam acts as a comp

6、etitive inhibitor and is not hydrolyzed by the b-lactamase 3.體內(nèi)研究 Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L insubjects 3. Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e02623-18. Antimicrob Agents Chemother. 2018 Jul 27;62(8)

7、. pii: e00414-18.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hecker SJ, et al. Discovery of a Cyclic Boronic Acid -Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. JMed Chem. 2015 May 14;58(9):3682-92.2. Castanheira M, et al. Effect of the -Lacta

8、mase Inhibitor Vaborbactam Combined with Meropenem against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8.3. Wong D, et al. Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy.McePdfHeightCaution: Product has not been fully validated for medical applications.F