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| 250mg |
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| 2g |
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| 5g |
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Purity: ≥98%
Imipenem belongs to the carbapenem class of antibiotics that is isolated from the soil organism Streptomyces cattleya, and is an intravenous β-lactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in 1980. It was the first member of the carbapenem class of antibiotics. Carbapenems are highly resistant to the β-lactamase enzymes produced by many multiple drug-resistant Gram-negative bacteria, and thus play a key role in the treatment of infections not readily treated with other antibiotics.
| ln Vivo |
Imipenem monohydrate (4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg, 64 mg/kg, IP, single dose) exhibits a time-dependent lethal effect [3]. Pharmacokinetic characteristics of imipenem monohydrate in neutropenic mice model of biofilm lung infection (4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg, 64 mg /kg, IP, single) [1]. 50 Drugs and dosage (mg/kg) Cmax (mg/L) Tmax (min) AUCtot (mg·min/L) Vz/F (ml/kg) Vss/F (ml/kg) CL/F (ml/min ) /kg) t1/2(min) MRT(min) Imipenem8 15 (7.1) 21 (11) 1,470 (777) 648 (330) 721 (343) 6.7 (3) 67 (11) 108 (12 ) 16 34 (6) 28 (18) 2,857 (559) 507 (140) 543 (121) 5.8 (1) 60 (9.1) 94 (10) 32 54 (11) 18 (6.1) 4,895 (635) 516 (75 ) 566 (83) ) 6.6 (0.8) 54 (6.5) 86 (11) 64 69 (37) 15 (9.5) 6,037 (2,976) 547 (274) 617 (308) 7.4 (3.6) 43 (22) 70 (35 )
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| Animal Protocol |
Animal/Disease Models: Neutropenic biofilm lung infection mouse model [3]
Doses: 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg, 64 mg/kg Doses: 4 mg/kg, 8 mg/kg, 16 mg/kg kg, 32 mg/kg, 64 mg/kg, IP, single Doses: Demonstrates time-dependent killing of mice infected with biofilm bacterial lungs effect. |
| References |
[1]. Johann Motsch, et al. RESTORE-IMI 1: A Multicenter, Randomized, Double-blind Trial Comparing Efficacy and Safety of Imipenem/Relebactam vs Colistin Plus Imipenem in Patients With Imipenem-nonsusceptible Bacterial Infections. Clin Infect Dis. 2020 Apr 15;70(9):1799-1808.
[2]. Wang Hengzhuang, et al. In vivo pharmacokinetics/pharmacodynamics of colistin and imipenem in Pseudomonas aeruginosa biofilm infection. Antimicrob Agents Chemother. 2012 May;56(5):2683-90 [3]. F P Tally, et al. In vitro activity of N-formimidoyl thienamycin (MK0787). Antimicrob Agents Chemother. 1980 Oct;18(4):642-4. |
| Molecular Formula |
C12H19N3O5S
|
|---|---|
| Molecular Weight |
317.3614
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| Elemental Analysis |
C, 45.42; H, 6.03; N, 13.24; O, 25.21; S, 10.10
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| CAS # |
74431-23-5
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| Related CAS # |
Imipenem;64221-86-9
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| Appearance |
Solid powder
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| SMILES |
O=C(C(N12)=C(SCC/N=C/N)C[C@]2([H])[C@@H]([C@H](O)C)C1=O)O.[H]O[H]
|
| InChi Key |
GSOSVVULSKVSLQ-JJVRHELESA-N
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| InChi Code |
InChI=1S/C12H17N3O4S.H2O/c1-6(16)9-7-4-8(20-3-2-14-5-13)10(12(18)19)15(7)11(9)17/h5-7,9,16H,2-4H2,1H3,(H2,13,14)(H,18,19)1H2/t6-,7-,9-/m1./s1
|
| Chemical Name |
(5R,6S)-3-((2-((E)-(aminomethylene)amino)ethyl)thio)-6-((R)-1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic
acid hydrate
|
| Synonyms |
Primaxin, MK-0787; MK 0787; MK0787; MK-787; MK787; MK 787; N-Formimidoylthienamycin; Tienamycin; Imipemide; Imipenem hydrate; Recarbrio;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~7.14 mg/mL (~22.50 mM )
DMSO : < 1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (31.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1510 mL | 15.7550 mL | 31.5100 mL | |
| 5 mM | 0.6302 mL | 3.1510 mL | 6.3020 mL | |
| 10 mM | 0.3151 mL | 1.5755 mL | 3.1510 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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