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Imipenem

亚胺培南
Catalog No.
P10075
 
组合的产品项目
规格价格库存 数量
10mg
¥ 272.00
现货
50mg
¥ 363.00
现货

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A

背景

Imipenem is one of the semisynthetic thienamycins with antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, which is stable to many beta-lactamases and shows a long half-life because of binding to plasma proteins [1].

Penicillin-binding proteins (PBPs) are a kind of membrane proteins, widely existing on the surface of bacteria, which is the main target site of beta-lactam antibiotics.

In E. coli and selected strains of P. aeruginosa, imipenem has shown to have the highest affinity to PBP-2, PBP-1a, and PBP-1b [2]. The inhibition of PBPs reduces the number of peptidoglycan polymer in the bacterial cell, thus prevent the forming of the bacterial cell wall and lead to cell death [3].

Reference:

[1] Zhanel G G, Wiebe R, Dilay L, et al. Comparative review of the carbapenems [J]. Drugs, 2007, 67(7): 1027-52.

[2] Nicolau D P. Carbapenems: a potent class of antibiotics [J]. Expert Opin Pharmacother. 2008, 9(1): 23-37.

[3] Brunton L L, Hilal-Dandan R, Knollmann B C. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt299.35
Cas No.64221-86-9
FormulaC12H17N3O4S
Solubilityinsoluble in EtOH; insoluble in DMSO; ≥29.9 mg/mL in H2O with gentle warming
Chemical Name(5R,6S)-3-[2-(aminomethylideneamino)ethylsulfanyl]-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESC[C@](O)([H])[C@](C1=O)([H])[C@@](N21)([H])CC(SCCNC=N)=C2C(O)=O
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试验操作

Cell experiment:[1]

Cell lines

Polymorphonuclear leucocytes (PMNs) and lymphomonocytes

Reaction Conditions

15, 30 and 60 mg/l imipenem

Applications

Preincubation of PMNs with the highest dosages (30 and 60 mg/l) was found to increase phagocytosis, while no effect was detected on superoxide anion production, as well as on lymphomonocyte proliferative response and cytokine production.

Animal experiment:[2]

Animal models

Male Sprague-Dawley rats aged 8 ~ 10 weeks and weighing 150 ~ 250 g, subjected to cecal ligation and puncture (CLP)

Dosage form

120 mg/kg

Injected intraperitoneally 6 h post-CLP and every 12 h for a total of 7 days

Applications

Imipenem combined with low-dose cyclophosphamide (CTX) could improve the survival rate of rats with sepsis compared with rats treated with imipenem alone. However, this combination significantly reduced IL-10 expression, potentially causing damage to the intestinal barrier function.

Note

The technical data provided above is for reference only.

References:

1. Pasqui AL, Di Renzo M, Bruni F, et al. Imipenem and immune response: in vitro and in vivo studies. Drugs under Experimental and Clinical Research, 1995, 21(1): 17-22.

2. Guo P, Zhang SW, Zhang J, et al. Effects of imipenem combined with low-dose cyclophosphamide on the intestinal barrier in septic rats. Experimental and Therapeutic Medicine, 2018, 16(3): 1919-1927.

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