Imipenem

目录号: GP11075纯度: >98%同义词: 亚胺培南

亚胺培南是一种半合成的硫霉素。

Cas No.: 64221-86-9

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Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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387(6739) (2025)
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387(6734) (2025)
Cell Research
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产品描述 Description

Imipenem is a semisynthetic thienamycin. Imipenem is one of the broad-spectrum antibiotics that has a bactericidal action against multiple gram-negative, gram-positive, aerobic, and anaerobic bacteria by binding to penicillin-binding protein 2 (PBP2) and interacting with bacterial cell wall synthesis^[2,5].It exerts a bactericidal effects by disrupting cell wall synthesis.

The MICs for the Y. pestis strains with imipenem ranged from a low of 0.12 mg/liter to a high of 1.0 mg/liter,the highest is 0.5 mg/liter^[7].Combination of relebactam with β-lactams led to >128- and 2-fold decreases in the MICs of amoxicillin and imipenem (from 8 to 4 mg/L). In vitro, M. abscessus was not killed by the imipenem/relebactam combination. In contrast, relebactam increased the intracellular activity of imipenem, leading to 88% killing^[6]. A high dose of imipenem enhanced the interleukin (IL)-1β level ^[9] and natural killer (NK) cell activity^[3].

Dose-dependent effect of subcutaneous administration of imipenem on the inflammatory responses in sepsis mice. A dose of 25 mg/kg imipenem resulted in better pathology, lower inflammatory mediators, and increased survival rate in sepsis mice^[1].

References:
[1]: Khosrojerdi A, Soudi S, et,al. Imipenem alters systemic and liver inflammatory responses in CLP- induced sepsis mice in a dose-dependent manner. Int Immunopharmacol. 2021 Apr;93:107421. doi: 10.1016/j.intimp.2021.107421. Epub 2021 Feb 4. PMID: 33548581.
[2]: Acar JF, Goldstein FW, et,al. Activity of imipenem on aerobic bacteria. J Antimicrob Chemother. 1983 Dec;12 Suppl D:37-45. doi: 10.1093/jac/12.suppl_d.37. PMID: 6421793.
[3]: Ortega E, de Pablo MA, et,al. Modification of natural immunity in mice by imipenem/cilastatin. J Antibiot (Tokyo). 1997 Jun;50(6):502-8. doi: 10.7164/antibiotics.50.502. PMID: 9268007.
[4]: Ortega E, de Pablo MA, et,al. Modification of acquired immunity in mice by imipenem/cilastatin. J Antimicrob Chemother. 1999 Oct;44(4):561-4. doi: 10.1093/jac/44.4.561. PMID: 10588322.
[5]: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Imipenem-Cilastatin. 2017 Jan 17. PMID: 31644018.
[6]: Le Run E, Atze H, et,al.Impact of relebactam-mediated inhibition of Mycobacterium abscessus BlaMab β-lactamase on the in vitro and intracellular efficacy of imipenem. J Antimicrob Chemother. 2020 Feb 1;75(2):379-383. doi: 10.1093/jac/dkz433. PMID: 31637424.
[7]: Heine HS, Louie A, et,al. Evaluation of imipenem for prophylaxis and therapy of Yersinia pestis delivered by aerosol in a mouse model of pneumonic plague. Antimicrob Agents Chemother. 2014 Jun;58(6):3276-84. doi: 10.1128/AAC.02420-14. Epub 2014 Mar 31. PMID: 24687492; PMCID: PMC4068467.

亚胺培南是一种半合成的硫霉素。亚胺培南是一种广谱抗生素，通过与青霉素结合蛋白 2 (PBP2) 结合并与细菌细胞壁合成相互作用，对多种革兰氏阴性菌、革兰氏阳性菌、需氧菌和厌氧菌具有杀菌作用^[2,5].通过破坏细胞壁合成发挥杀菌作用。

鼠疫耶尔森菌株与亚胺培南的 MIC 范围从最低的 0.12 毫克/升到最高的 1.0 毫克/升，最高为 0.5 毫克/升^[7]。组合relebactam 和 β-内酰胺导致 &gt；阿莫西林和亚胺培南的 MIC 分别降低 128 倍和 2 倍（从 8 mg/L 到 4 mg/L）。在体外，亚胺培南/relebactam 组合未杀死脓肿分枝杆菌。相比之下，relebactam 增加了亚胺培南的细胞内活性，导致 88% 的杀灭^[6]。高剂量亚胺培南可增强白细胞介素 (IL)-1β 水平^[9]和自然杀伤 (NK) 细胞活性^[3]。

亚胺培南皮下给药对脓毒症小鼠炎症反应的剂量依赖性影响。 25 mg/kg 亚胺培南的剂量可改善脓毒症小鼠的病理学、降低炎症介质并提高存活率^[1]。

实验参考方法 Experimental Reference Method

MIC experiment [1]:
Preparation Method	Susceptibilities of Y. pestis strains were determined by the broth microdilution method according to CLSI M45-A2
Reaction Conditions	0.04-2mg/L imipenem in 35°C
Applications	The MICs for the Y. pestis strains with imipenem ranged from a low of 0.12 mg/liter to a high of 1.0 mg/liter，the higher is 0.5 mg/liter
Cell experiment[2]:
Cell experiment	THP-1 cells
Preparation Method	THP-1 cells were seeded into 24-well plates, differentiated for 24 h and infected with M. abscessus CIP104536. Imipenem (8 and 32 mg/L) or amoxicillin alone or in combination with relebactam (16 mg/L) or avibactam (16 mg/L) were added to each well. Rifabutin was also studied in combination with imipenem (8 mg/L), imipenem/relebactam or imipenem/avibactam. Imipenem was added every 24 h.
Reaction Conditions	Imipenem (8 and 32 mg/L) was added every 24 h.
Applications	Combination of relebactam with β-lactams led to >128- and 2-fold decreases in the MICs of amoxicillin and imipenem (from 8 to 4 mg/L). In vitro, M. abscessus was not killed by the imipenem/relebactam combination. In contrast, relebactam increased the intracellular activity of imipenem, leading to 88% killing.
Animal experiment [3]:
Animal models	Female C57BL/6 mice (6-8 weeks old, 20-25 g body weight)
Preparation Method	Mice were randomly divided into four groups: the sham-operated mice as the control group, CLP-induced sepsis mice, CLP-induced sepsis mice treated with the low dose of imipenem (25 mg/kg), CLP-induced sepsis mice treated with the high dose of imipenem (125 mg/kg). Imipenem was injected one hour after sepsis induction, repeating the injection every 24 h up to 72 h.
Dosage form	25-200 mg/kg imipenem, repeating the injection every 24 h up to 72 h.
Applications	Sepsis mice treated with a high dose (125 mg/kg) of imipenem showed a significant reduction in bacterial load, while increased liver enzymes, endotoxin level, and inflammatory cytokine production in plasma and liver. Significant reduction in the liver enzymes, bacterial load, endotoxin levels, and inflammatory cytokine levels was observed in the mice treated with a low dose (25 mg/kg) of imipenem. Liver tissue pathology of mice indicated little tissue destruction in the sepsis mice treated with 25 mg/kg of imipenem compared to other groups. Mice receiving 25 mg/kg of imipenem had better survival rate.
References: [1]. Heine HS, Louie A, et,al. Evaluation of imipenem for prophylaxis and therapy of Yersinia pestis delivered by aerosol in a mouse model of pneumonic plague. Antimicrob Agents Chemother. 2014 Jun;58(6):3276-84. doi: 10.1128/AAC.02420-14. Epub 2014 Mar 31. PMID: 24687492; PMCID: PMC4068467. [2]. Le Run E, Atze H, et,al. Impact of relebactam-mediated inhibition of Mycobacterium abscessus BlaMab β-lactamase on the in vitro and intracellular efficacy of imipenem. J Antimicrob Chemother. 2020 Feb 1;75(2):379-383. doi: 10.1093/jac/dkz433. PMID: 31637424. [3]. Khosrojerdi A, Soudi S, et,al. Imipenem alters systemic and liver inflammatory responses in CLP- induced sepsis mice in a dose-dependent manner. Int Immunopharmacol. 2021 Apr;93:107421. doi: 10.1016/j.intimp.2021.107421. Epub 2021 Feb 4. PMID: 33548581.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

64221-86-9

同义词

亚胺培南

化学名

(5R,6S)-3-[2-(aminomethylideneamino)ethylsulfanyl]-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid

SMILES

C[C@](O)([H])[C@](C1=O)([H])[C@@](N21)([H])CC(SCCNC=N)=C2C(O)=O

分子式

C₁₂H₁₇N₃O₄S

分子量

299.35 g/mol

溶解性

Water: 63 mg/mL; DMSO: 1 mg/mL (3.15 mM; DMSO moisture absorption will reduce compound solubility, please use newly opened DMSO); Ethanol: Insoluble

保存条件

Store at -20°C

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°C，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。

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