Ertapenem disodium

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Ertapenem disodium

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。

CAS NO:

153832-38-3

MK-0826 disodium

Ertapenem (MK-0826) disodium 是一种广谱的长效 β-内酰胺抗生素。Ertapenem disodium 对多种厌氧菌具有广谱抗菌活性，其 MIC 值为 0.12 μg/mL。Ertapenem disodium 可用于皮肤、肺、胃、骨盆和泌尿道的细菌感染相关的研究。

生物活性

Ertapenem (MK-0826) disodium is a broad spectrum and long acting β-lactamantibiotic. Ertapenem disodium has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem disodium can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract^[1]^[2].

IC₅₀& Target

β-lactam

体外研究
(In Vitro)

Ertapenem disodium (0-100 μg/mL approximately, 48 h) is active against 99.1% of all anaerobes with a mode MIC of 0.12 μg/mL and MIC₉₀of 1 μg/mL, and MIC’s ≥8 μg/mL forB.fragilisandB.vulgatusspecies, respectively^[1].

Cell Viability Assay^[1]

Cell Line:	B. fragilis(ATCC 25285),B. thetaiotaomicron(ATCC 29741), andEubacterium lentum(ATCC 43055)
Concentration:	0-100 μg/mL approximately
Incubation Time:	48 h
Result:	Inhibited 99.1% of all isolate with a mode MIC of 0.12 μg/mL and MIC₉₀of 1 μg/mL, and 98.8% of the isolates were susceptible among the B. fragilis group.

体内研究
(In Vivo)

Ertapenem disodium (Subcutaneous injection, 0-10 mg/kg, 0-120 h after infection,S. aureusthigh tissue infection model) shows >3 log₁₀CFU reduction of organism at 10 mg/kg, and maintains the activity with 3.3 and 4.4 log₁₀CFU eliminated at 2 mg/kg^[2].
Ertapenem disodium (Subcutaneous injection, 4h after infection, systemic infection model) is active against all gram-positive organisms, and is also active against gram-negative organisms tested with ED₅₀s of<0.25 mg/kg/dose^[2].

Animal Model:	S. aureusthigh tissue infection model (DBA/2 mice)^[2]
Dosage:	0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10, 24, 48, 72, 96, 120 h)
Administration:	Subcutaneous injection (0.5 mL after infection)
Result:	Displayed >3 log₁₀CFU reduction of organism compared to non-antibiotic-treated controls at 10 mg/kg. Maintained the activity with 3.3 and 4.4 log₁₀CFU eliminated at 2 mg/kg.

Animal Model:	Systemic infection model (DBA/2 female mice, viral antibody-free CD-1 female mice)^[2]
Dosage:	0-3 mg/kg approximately
Administration:	Subcutaneous injection (0.5 mL, begin immediately and 4 h after infection)
Result:	Showed activity against all gram-positive organisms, and also ram-negative organisms tested with ED₅₀s of<0.25 mg/kg/dose.

Animal Model:	CD-1 mice, rats^[2]
Dosage:	10 mg/kg approximately
Administration:	Intraperitoneal injection (pharmacokinetic assay)
Result:	Exhibited an AUC_0-∞ranging from 1.8-21.82 μgohr/mL in tissue in mice following a 10-mg/kg i.p. dose. Exhibited slow clearance rate with a t_1/2βof 3.2 h, Clp of 0.47 mL/min/kg, AUC_0-8of 284.15μgohr/mL.

Clinical Trial

分子量

519.48

Formula

C₂₂H₂₃N₃Na₂O₇S

CAS 号

153832-38-3

中文名称

厄他培南

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.