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Durlobactam Triethylamine

产品编号 T25355L

别名: Durlobactam Triethylamine(1467829-71-5 Free base), ETX 2514 Triethylamine, ETX-2514 Triethylamine, ETX2514 Triethylamine

Durlobactam Triethylamine (ETX2514 Triethylamine) 是一种二氮杂双环辛烷β-内酰胺酶抑制剂，可抑制 A、C 和 D 类β-内酰胺。Durlobactam Triethylamine 具有抗真菌感染活性。

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Durlobactam Triethylamine Chemical Structure

Durlobactam Triethylamine, CAS N/A

规格	价格/CNY	货期
5 mg	￥ 9,890	待询
10 mg	￥ 13,800	待询
25 mg	￥ 14,500	待询
50 mg	￥ 19,980	待询
100 mg	￥ 26,400	待询

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选择批次

纯度: 97.39%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述

Durlobactam Triethylamine (ETX2514 Triethylamine) is a diazabicyclooctane β-lactamase inhibitor that inhibits classes A, C, and D β-lactams.Durlobactam Triethylamine has antifungal infection activity.

体内活性

This was a phase 1 study to evaluate the effects of various degrees of renal impairment, including subjects with end-stage renal disease (ESRD) on hemodialysis (HD), on the pharmacokinetics and safety profile of Durlobactam (also known as ETX2514) and sulbactam after single intravenous (i.v.) dose administration. For healthy subjects and those with mild or moderate renal impairment (RI), single 1,000-mg doses each of Durlobactam and sulbactam via a 3-h i.v. infusion was administered, and for severe renal impairment, 500mg doses were administered. For subjects with ESRD and HD, 500 mg i.v. doses of Durlobactam and sulbactam were administered post-HD and pre-HD, with a 1-week washout between doses. Among 34 subjects, decreasing renal function increased systemic exposure (peak plasma concentration [Cmax] and area under the concentration-time curve [AUC]) to Durlobactam and sulbactam in a generally linear manner. In healthy subjects and in those with mild or moderate renal impairment, the majority of Durlobactam and sulbactam was excreted in the urine, while approximately 40% or less was excreted in the urine in subjects with severe renal impairment or ESRD. In subjects with ESRD, hemodialysis was effective at removing both Durlobactam and sulbactam from plasma. Renal impairment had no effect on the safety/tolerability profile of Durlobactam and sulbactam. In summary, RI and ESRD had a predictable effect on the pharmacokinetic (PK) profile of Durlobactam and sulbactam with no adverse effects on the safety/tolerability profile. Durlobactam and sulbactam are cleared to a similar extent by renal elimination and are impacted similarly by renal impairment. The results from this study have been used with population PK modeling and non-clinically derived PK/PD (pharmacodynamic) exposure targets to establish dosage recommendations for Durlobactam and sulbactam in patients with various degrees of RI. The dosing regimen of Durlobactam-sulbactam will require adjustment in patients with severe renal insufficiency and in those with ESRD.[1]

别名	Durlobactam Triethylamine(1467829-71-5 Free base), ETX 2514 Triethylamine, ETX-2514 Triethylamine, ETX2514 Triethylamine
分子量	378.44
分子式	C14H26N4O6S

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. O'Donnell J, et al. Pharmacokinetics, Safety, and Tolerability of Intravenous Durlobactam and Sulbactam in Subjects with Renal Impairment and Healthy Matched Control Subjects. Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00794-19. 2. Granata G, et al. Durlobactam in the Treatment of Multidrug-Resistant Acinetobacter baumannii Infections: A Systematic Review. J Clin Med. 2022 Jun 7;11(12):3258.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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