Imipenem |
Catalog No.GP11075
One-Click Copy Product Info
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Imipenem is a semisynthetic thienamycin.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64221-86-9
Sample solution is provided at 25 µL, 10mM.
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]. Imipenem exerts a bactericidal effects by disrupting cell wall synthesis.
In vitro, the MICs of imipenem against the Y. pestis strains ranged from 0.12 to 1.0mg/L[6].
In vivo, Imipenem (4g/70kg/day; i.p.; 7 days) decreased peritoneal cell counts and phagocytic activity, but increased IL-1 production and NK cell activity in BALB/c mice[3]. Imipenem (125mg/kg; s.c.; every 24h for 72h) significantly reduced bacterial load, but increased liver enzymes, endotoxin levels, and inflammatory cytokine production in the plasma and liver of septic mice[1]. Imipenem (25mg/kg; s.c.; every 24h for 72h) significantly reduced liver enzymes, bacterial load, endotoxin levels, and inflammatory cytokine levels in septic 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] 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.
| MIC experiment [1]: | |
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Preparation Method |
Susceptibilities of Y. pestis strains were determined by the broth microdilution method according to CLSI M45-A2 |
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Reaction Conditions |
0.04-2mg/L; 35°C |
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Applications |
The MICs for the Y. pestis strains with Imipenem ranged from a low of 0.12mg/liter to a high of 1.0mg/liter. |
| Cell experiment[2]: | |
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Cell experiment |
THP-1 cells |
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Preparation Method |
THP-1 cells were seeded into 24-well plates, differentiated for 24h and infected with M. abscessus CIP104536. Imipenem (8 and 32mg/L) or amoxicillin alone or in combination with relebactam (16mg/L) or avibactam (16mg/L) were added to each well. Rifabutin was also studied in combination with imipenem (8mg/L), Imipenem/relebactam or Imipenem/avibactam. Imipenem was added every 24h. |
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Reaction Conditions |
8 and 32mg/L; 24h |
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Applications |
Combination of relebactam with β-lactams led to >128- and 2-fold decreases in the MICs of amoxicillin and Imipenem (from 8 to 4mg/L). 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]: | |
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Animal models |
Female C57BL/6 mice (6-8 weeks old, 20-25g body weight) |
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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 (25mg/kg), CLP-induced sepsis mice treated with the high dose of Imipenem (125mg/kg). Imipenem was injected one hour after sepsis induction, repeating the injection every 24h up to 72h. |
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Dosage form |
25 or 125mg/kg; s.c; repeating the injection every 24h up to 72h |
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Applications |
Sepsis mice treated with a high dose (125mg/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 (25mg/kg) of Imipenem. Liver tissue pathology of mice indicated little tissue destruction in the sepsis mice treated with 25mg/kg of Imipenem compared to other groups. Mice receiving 25mg/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 ?-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. | |
| Cas No. | 64221-86-9 | SDF | |
| 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 | ||
| Canonical SMILES | C[C@](O)([H])[C@](C1=O)([H])[C@@](N21)([H])CC(SCCNC=N)=C2C(O)=O | ||
| Formula | C12H17N3O4S | M.Wt | 299.35 |
| Solubility | 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 | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3406 mL | 16.7029 mL | 33.4057 mL |
| 5 mM | 668.1 μL | 3.3406 mL | 6.6811 mL |
| 10 mM | 334.1 μL | 1.6703 mL | 3.3406 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)