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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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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 |
Time-dependent death is the effect of imipenem (MK0787) (4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg, 64 mg/kg, IP, single dose) [3]. Ipenem's pharmacokinetic properties (4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg, 64 mg/kg, IP,single) in a neutropenic mouse biofilm lung infection model[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]. F P Tally, et al. In vitro activity of N-formimidoyl thienamycin (MK0787). Antimicrob Agents Chemother. 1980 Oct;18(4):642-4. [3]. 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. |
Molecular Formula |
C12H17N3O5S
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Molecular Weight |
299.3461
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CAS # |
64221-86-9
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Related CAS # |
Imipenem monohydrate;74431-23-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(O)OC(N12)=C(SCCNC=N)C[C@]2([H])[C@@H]([C@H](O)C)C1=O
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InChi Key |
VBTPAOZKIGVELK-ZXFLCMHBSA-N
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InChi Code |
InChI=1S/C12H17N3O5S/c1-6(16)9-7-4-8(21-3-2-14-5-13)11(20-12(18)19)15(7)10(9)17/h5-7,9,16H,2-4H2,1H3,(H2,13,14)(H,18,19)/t6-,7-,9-/m1/s1
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Chemical Name |
(5R,6S)-6-((R)-1-Hydroxyethyl)-3-(2-(iminomethylamino)ethylthio)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carbonsaeure
hydrate
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3406 mL | 16.7029 mL | 33.4057 mL | |
5 mM | 0.6681 mL | 3.3406 mL | 6.6811 mL | |
10 mM | 0.3341 mL | 1.6703 mL | 3.3406 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.