名称 | Durlobactam sodium salt |
描述 | Durlobactam sodium salt (ETX2514) is a beta-lactamase inhibitor with IC50 values of 4 nM, 14 nM and 190 nM against class A KPC-2, class C AmpC and class D OXA-24. |
体外活性 | Method: After pre-incubation of Durlobactam sodium salt (ETX2514) with enzyme for 5 minutes, the IC50 value of Durlobactam for representative class A, C and D β-lactamases was measured.
RESULTS The IC50 values of Durlobactam against Class A KPC-2, Class C AmpC, and Class D OXA-24 are 0.004μM, 0.014μM and 0.19μM respectively. [1]
METHODS: Antimicrobial susceptibility testing of BCC and B. gladioli clinical isolates was performed with Durlobactam (2-64 μg/ml).
RESULTS Durlobactam showed moderate activity (MIC90= 16 μg/ml). [2] |
体内活性 | METHODS: Subjects were randomly assigned to 1 of 6 sequences, including a single 3-hour intravenous infusion of Durlobactam sodium salt (ETX2514) 4 g, a single 3-hour intravenous infusion of placebo, and a single 3-hour intravenous infusion of placebo plus a single dose. The second oral dose of moxifloxacin 400 mg was given open label at the end of the intravenous infusion. During each treatment period, ambulatory electrocardiogram (ECG) measurements were obtained from before dosing to 24 hours after the start of infusion.
RESULTS Durlobactam had no significant effect on electrocardiographic parameters, including QT interval prolongation. Durlobactam carries a low risk of prolonging the QT interval and is unlikely to produce any proarrhythmic effects. [3] |
存储条件 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (167.1 mM) H2O : 2.5 mg/mL (8.35 mM), Sonication is recommended.
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关键字 | ETX-2514 | ETX 2514 | Durlobactam sodium |
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