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Meropenem

现货
Catalog No.
A5124
β-内酰胺抗生素
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
25mg
¥ 500.00
现货
50mg
¥ 600.00
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100mg
¥ 900.00
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250mg
¥ 1,800.00
现货

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Background

Meropenem is an ultra-broad-spectrum injectable β-lactam antibiotic used to treat a wide variety of infections. Meropenem has been shown to inhibit penicillinase-negative, -positive and methicillin-susceptible staphylococci [1].

In vitro: The meropenem MICs for penicillin-resistant Streptococcus pneumoniae were higher than for the penicillin-susceptible strains but the organisms remained susceptible. Clinical susceptibility in vitro to meropenem was defined by MICs of ≤ 4 mg/L, intermediate susceptibility by MICs of 8 mg/L and MICs of ≥ 16 mg/L define resistance; equivalent figures for zones of growth inhibition were ≥ 14 (susceptible), 12-13 (intermediate) and ≤ 11 (resistant) mm[1].Meropenem was 2- to 4-fold more active than imipenem against Gram-negative organisms and its spectrum of antimicrobial activity was wider than those of all other drugs tested.Meropenem inhibited all anaerobic bacteria at less than or equal to 8 mg/l and 0.25 mg/l inhibited 50% of strains. Meropenem MICs were not significantly influenced by high inocula and the drug was generally bactericidal [2].Meropenem bound most strongly to penicillin-binding protein 2 of Escherichia coli and Pseudomonas aeruginosa, and to penicillin-binding proteins 1 of Staphylococcus aureus [3].Meropenem had one identified metabolite, a β-lactam ring-opened form which is devoid of microbiological activity[4].

In vivo: In rabbits, meropenem significantly increased the plamsa total clearance of valproate to about 1.5 times compared to the control (6.09 mL/min/kg vs. 4.28 mL/min/kg). Meropenem significantly increased the urinary excretion of valproate- glucuronide in rabbits [5].

References:
[1].  Edwards J R. Meropenem: a microbiological overview[J]. Journal of Antimicrobial Chemotherapy, 1995, 36(suppl A): 1-17.
[2].  Jones R N, Barry A L, Tbornsberry C. In-vitro studies of meropenem[J]. Journal of Antimicrobial Chemotherapy, 1989, 24(suppl A): 9-29.
[3].  Yang Y, Bhachech N, Bush K. Biochemical comparison of imipenem, meropenem and biapenem: permeability, binding to penicillin-binding proteins, and stability to hydrolysis by β-lactamases[J]. Journal of Antimicrobial Chemotherapy, 1995, 35(1): 75-84.
[4].  Drusano G L, Hutchison M. The pharmacokinetics of meropenem[J]. Scandinavian journal of infectious diseases.Supplementum, 1994, 96: 11-16.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt383.46
Cas No.96036-03-2
FormulaC17H25N3O5S
Solubility≥19.15mg/mL in DMSO, <2.34 mg/mL in EtOH, ≥9.88 mg/mL in H2O with ultrasonic
Chemical Name(4R,5S,6S)-3-[(3S,5S)-5-(dimethylcarbamoyl)pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1C2C(C(=O)N2C(=C1SC3CC(NC3)C(=O)N(C)C)C(=O)O)C(C)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

1116株,其中包括659种革兰氏阴性细菌,271种革兰阳性菌,96株罕见分离物种和90种严格的厌氧菌。

溶解方法

该化合物在DMSO中的溶解度>19.2mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0-25 mg/l

应用

在659种革兰氏阴性细菌中,Meropenem对这些列出的物种展示出最广泛的活性,抑制除9种菌株(MIC≥16mg/ l)以外的所有物种。在测试的271种革兰阳性生物中,只有两种耐甲氧西林葡萄球菌和5种屎肠球菌菌株的meropenem MICs为≥16mg/ l。在90种严格厌氧生物菌株中,Meropenem对这些细菌相当活跃,总体MIC90为1mg / l。

动物实验[2]:

动物模型

肺炎克雷伯杆菌败血症大鼠模型

剂量

30mg/kg和等效剂量的载药纳米颗粒分散体; 单次腹腔注射

应用

在肺炎克雷伯杆菌的败血症大鼠模型中,与对照未处理的大鼠(50%死亡率)相比,用游离meropenem治疗的死亡率为30%,无统计学显著性。然而,用负载药物的纳米颗粒分散体处理的所有大鼠在48小时内存活,表明存活率显著改善。用游离meropenem治疗的感染动物没有显示血细菌计数的显著降低,而药物负载的纳米颗粒显著降低血液细菌计数。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Jones R N, Barry A L, Tbornsberry C. In-vitro studies of meropenem[J]. Journal of Antimicrobial Chemotherapy, 1989, 24(suppl A): 9-29.

[2]. Abdelkader A1, El-Mokhtar MA2, Abdelkader O1, et al. Ultrahigh antibacterial efficacy of meropenem-loaded chitosan nanoparticles in a septic animal model. Carbohydr Polym. 2017 Oct 15;174:1041-1050.

质量控制

化学结构

Meropenem