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Ertapenem(sodium salt)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ertapenem(sodium salt)图片
CAS NO:153832-38-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Ertapenem (MK-0826) disodium 是一种广谱长效 β-lactam 抗生素。
Cas No.153832-38-3
别名厄他培南钠,L-749
化学名(4R,5S,6S)-3-[[(3S,5S)-5-[[(3-carboxyphenyl)amino]carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, disodium salt
Canonical SMILESO=C1[C@@]([C@@H](C)O)([H])[C@]2([H])N1C(C([O-])=O)=C(S[C@@H]3CN[C@H](C(NC4=CC(C([O-])=O)=CC=C4)=O)C3)[C@@H]2C.[Na+].[Na+]
分子式C22H23N3O7S o 2Na
分子量519.5
溶解度≥ 52mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ertapenem, the first group of carbapenems, is a 1-β-methyl carbapenem with potent in vitro activity against a broad spectrum of bacterial pathogens including Gram-positive and Gram-negative aerobic and anaerobic pathogens [1].

In vitro: In E.coli, ertapenem binds to penicillin binding proteins (PBPs) 1a, 1b, 2, 3, 4 and 5, showing highest affinity for PBPs 2 and 3 [1]. MIC90s for most species of Enterobacteriaceae were< 1 mg/L. MIC90s for most Bacteroides fragilis group isolates ranged from 1 to 4 mg/L, and MIC90s were species specific for Clostridium, ranging from 0.06 mg/L for Clostridium perfringens to 4 mg/L for Clostridiumclostridioforme [2].

In vivo: In healthy young men and women volunteers, the mean concentration of ertapenem in plasma ranged from ~145 to 175 μg/ml at the end of a 30-min infusion, from ~30 to 34 μg/ml at 6 h, and from ~9 to 11 μg/ml at 12 h. The mean plasma t1/2 ranged from 3.8 to 4.4 h. About 45% of the plasma clearance (CLP) was via renal clearance [3].

Clinical trials: Ertapenem was highly effective in patients with a range of disease severity within each indication, including elderly patients and patients with severe infections. Ertapenem is not hepatically metabolized and is primarily eliminated by the renal route; dose reduction to 0.5 g once a day is required in patients with severe renal insufficiency. Ertapenem is rapidly bactericidal. The most common adverse reactions reported with ertapenem were diarrhoea, nausea, infused vein complication, vaginitis, headache in females, phlebitis/thrombophlebitis, vomiting and elevated aminotransferase levels.

References:
[1].  Shah P M, Isaacs R D. Ertapenem, the first of a new group of carbapenems[J]. Journal of antimicrobial Chemotherapy, 2003, 52(4): 538-542.
[2].  Wexler H M. In vitro activity of ertapenem: review of recent studies[J]. Journal of Antimicrobial Chemotherapy, 2004, 53(suppl 2): ii11-ii21.
[3].  Majumdar A K, Musson D G, Birk K L, et al. Pharmacokinetics of ertapenem in healthy young volunteers[J]. Antimicrobial Agents and Chemotherapy, 2002, 46(11): 3506-3511.