Ertapenem sodium (L-749345)
(Synonyms: 厄他培南钠; L-749345; MK-826) 目录号 : GC32101
Ertapenem sodium (L-749345)是一种碳青霉烯类的β-内酰胺抗生素,其MIC众数为0.12μg/ml,对需氧和厌氧微生物都具有活性。
Cas No.:153773-82-1
Sample solution is provided at 25 µL, 10mM.
Ertapenem sodium (L-749345) is a β-lactam antibiotic of the carbapenem class with a modal MIC of 0.12μg/ml, which is active against both aerobic and anaerobic microorganisms[1-2]. Ertapenem sodium is highly stable against nearly all beta-lactamases, including AmpC and extended-spectrum beta-lactamases, except metallo-β-lactamases[3-4].
In vitro, using the broth microdilution method, 99.1% of the 556 clinical anaerobic isolates were inhibited by Ertapenem sodium at a concentration of 4μg/ml, with a modal MIC of 0.12μg/ml[1]. By using an agar dilution method, the comparative in vitro activities of Ertapenem sodium were studied against 1,001 anaerobes isolated from human intra-abdominal infections in 17 countries worldwide. Ertapenem sodium was uniformly active against all isolates, including all Bacteroides fragilis group species isolates, except for 12 of 61 (20%) strains of Bilophila wadsworthia, 3 strains of lactobacilli, and 1 isolate of Acidaminococcus fermentans[5].
In vivo, after a single intraperitoneal injection of Ertapenem sodium (10mg/kg of body weight) to CD-1 mice, the CFU of Staphylococcus aureus in the mice decreased[6]. After intravenous administration of Ertapenem sodium (10-180mg/kg) in rats, Ertapenem sodium exhibited extensive plasma protein binding in rat plasma, with the extent of binding being concentration-dependent at the plasma concentrations achieved following these doses[7].
References:
[1] Aldridge KE. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002;44(2):181-186.
[2] Pedroso TM, Salgado HR. A Critical Review of Analytical Methods for Determination of Ertapenem Sodium. Crit Rev Anal Chem. 2016;46(1):15-21.
[3] Parakh A, Krishnamurthy S, Bhattacharya M. Ertapenem. Kathmandu Univ Med J (KUMJ). 2009;7(28):454-460.
[4] Kilińska K, Cielecka-Piontek J, Skibiński R, et al. The Radiation Sterilization of Ertapenem Sodium in the Solid State. Molecules. 2019;24(16):2944.
[5] Goldstein EJ, Citron DM, Vreni Merriam C, Warren Y, Tyrrell KL. Comparative In vitro activities of ertapenem (MK-0826) against 1,001 anaerobes isolated from human intra-abdominal infections. Antimicrob Agents Chemother. 2000;44(9):2389-2394.
[6] Gill CJ, Jackson JJ, Gerckens LS, et al. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998;42(8):1996-2001.
[7] Wong BK, Bruhin PJ, Lin JH. Dose-dependent plasma clearance of MK-826, a carbapenem antibiotic, arising from concentration-dependent plasma protein binding in rats and monkeys. J Pharm Sci. 1999;88(2):277-280.
Ertapenem sodium (L-749345)是一种碳青霉烯类的β-内酰胺抗生素,其MIC众数为0.12μg/ml,对需氧和厌氧微生物都具有活性[1-2]。Ertapenem sodium对几乎所有β-内酰胺酶(包括AmpC和广谱β-内酰胺酶)都非常稳定,但对金属β-内酰胺酶除外[3-4]。
在体外,采用肉汤微量稀释法,99.1%的556株临床厌氧菌分离株被Ertapenem sodium在4μg/ml的浓度下抑制,其MIC众数为0.12μg/ml[1]。采用琼脂稀释法,研究了Ertapenem sodium对来自全球17个国家的人类腹腔内感染的1001株厌氧菌的体外活性。Ertapenem sodium对所有菌株,包括所有脆弱拟杆菌群种的菌株,均表现出均匀的活性,但有61株沃氏双叶菌中的12株(20%)、3株乳杆菌和1株发酵酸胺菌例外[5]。
在体内,对CD-1小鼠进行单次腹腔注射Ertapenem sodium(10mg/kg体重)后,小鼠体内金黄色葡萄球菌的CFU减少[6]。在大鼠中静脉注射Ertapenem sodium(10-180mg/kg)后,Ertapenem sodium在大鼠血浆中与血浆蛋白广泛结合,且在这些剂量给药后达到的血浆浓度下,结合程度呈浓度依赖性[7]。
In vitro experiment [1]: | |
materials | isolates of Prevotella, Porphyromonas, Fusobacterium, and Peptostreptococcus |
Preparation Method | Susceptibility testing was done by a broth microdilution method, using Anaerobe broth MIC as the test medium with an inoculum size of 105 CFU per well, and incubation time of 48h in an anaerobe chamber. MIC values were read as the lowest concentration (μg/mL) of Ertapenem sodium that inhibited the growth of the test isolate. Breakpoints (μg/ml) for eErtapenem sodium were≤4 as S, 8 as I, and≥16 as R. |
Reaction Conditions | 0.015-32μg/mL |
Applications | All isolates of Prevotella, Porphyromonas, Fusobacterium, and Peptostreptococcus were susceptible to Ertapenem sodium. |
Animal experiment [2]: | |
Animal models | Female Sprague-Dawley rats |
Preparation Method | Female Sprague-Dawley rats were anesthetized i.p. with ∼50mg of pentobarbitol sodium per kg. A small horizontal incision (3 to 4cm) was made below the xiphoid process. The bile duct was exposed and a cannula of Silastic tubing was threaded into the duct and anchored with ligatures. The abdominal incision was closed with stainless steel wound clips. To facilitate blood collection, an incision was made in the right hind leg of the rat, exposing the femoral artery. A sterile PE 10 catheter was fed into the abdominal aorta and secured in place with silk ligatures. Once normal bile flow was established, each rat was given an s.c. dose of cilastatin (40mg/kg) followed by an intravenous (i.v.) injection of Ertapenem sodium in the femoral artery at a dose equivalent to 10mg/kg. Heparinized blood samples were taken at 5, 30, 60, 120, 240, 360, and 480min postdose. |
Dosage form | 40mg/kg; s.c. |
Applications | Ertapenem sodium was cleared very slowly from the plasma of all three rats. An average concentration of 15.10μg/ml remained 8h posttreatment, with the β-terminal elimination plasma t1/2 (t1/2β) averaging 3.2h and the plasma clearance (Clp) averaging 0.47ml/min/kg. |
References: |
Cas No. | 153773-82-1 | SDF | |
别名 | 厄他培南钠; L-749345; MK-826 | ||
Canonical SMILES | O=C([C@H]1NC[C@@H](SC2=C(C(O)=O)N3[C@]([C@]([C@@H](C)O)([H])C3=O)([H])[C@H]2C)C1)NC4=CC=CC(C([O-])=O)=C4.[Na+] | ||
分子式 | C22H24N3NaO7S | 分子量 | 497.5 |
溶解度 | Water : 50 mg/mL (100.50 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
![]() |
1 mg | 5 mg | 10 mg |
1 mM | 2.0101 mL | 10.0503 mL | 20.1005 mL |
5 mM | 0.402 mL | 2.0101 mL | 4.0201 mL |
10 mM | 0.201 mL | 1.005 mL | 2.0101 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet