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Ertapenem disodium (MK-0826) is a long acting β-lactam antibiotic with a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. It is used for the treatment of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract.
| Targets |
β-lactam
|
|---|---|
| ln Vitro |
In roughly 48 hours, ertapenem disodium (0-100 μg/mL) can effectively combat 99.1% of anaerobes, as demonstrated by its mode MIC of 0.12 μg/mL, MIC90 of 1 μg/mL, and MICs of ≥8 μg/mL for B.fragilis and B. vulgatus species, respectively[1].
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| ln Vivo |
Using the S. aureus thigh tissue infection model, ertapenem disodium (subcutaneous injection, 0–10 mg/kg, 0-120 h after infection) reduces the organism by > 3 log10 CFU at 10 mg/kg and keeps the activity at 3.3 and 4.4 log10 CFU removed at 2 mg/kg[2]. In addition to being efficacious against all gram-positive species, ertapenem disodium (subcutaneous injection, 4 hours after infection, systemic infection model) is also active against gram-negative organisms with ED50s of less than 0.25 mg/kg/dose[2].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: B. fragilis (ATCC 25285), B. thetaiotaomicron (ATCC 29741), and Eubacterium lentum (ATCC 43055) Tested Concentrations: 0-100 μg/ mL approximately Incubation Duration: 48 h Experimental Results: Inhibited 99.1% of all isolate with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL, and 98.8% of the isolates were susceptible among the B. fragilis group. |
| Animal Protocol |
Animal/Disease Models: S. aureus thigh tissue infection model (DBA/2 mice)[2]
Doses: 0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10 , 24, 48, 72, 96, 120 h) Route of Administration: subcutaneous (sc) injection (0.5 mL after infection) Experimental Results: Displayed > 3 log10 CFU reduction of organism compared to non-antibiotic-treated controls at 10 mg/kg. Maintained the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg. Animal/Disease Models: Systemic infection model (DBA/2 female mice, viral antibody-free CD-1 female mice)[2] Doses: 0-3 mg/kg approximately Route of Administration: subcutaneous (sc) injection (0.5 mL, begin immediately and 4 h after infection) Experimental Results: demonstrated activity against all gram-positive organisms, and also ram-negative organisms tested with ED50s of <0.25 mg/kg/dose. Animal/Disease Models: CD-1 mice, rats[2] Doses: 10 mg/kg approximately Route of Administration: intraperitoneal (ip)injection (pharmacokinetic/PK assay) Experimental Results: demonstrated an AUC0-∞ ranging from 1.8-21.82 μg·hr/mL in tissue in mice following a 10-mg/kg ip dose. demonstrated slow |
| References |
[1]. Kenneth E Aldridge. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002 Oct;44(2):181-6.
[2]. C J Gill, et al. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998 Aug;42(8):1996-2001. |
| Additional Infomation |
Ertapenem Sodium is the sodium salt of ertapenem, a 1-beta-methyl carbapenem and a broad-spectrum beta-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death. In vitro, this agent has shown activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases.
A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery. |
| Molecular Formula |
C22H23N3NA2O7S
|
|---|---|
| Molecular Weight |
519.48
|
| Exact Mass |
497.1232
|
| CAS # |
153832-38-3
|
| Related CAS # |
Ertapenem sodium;153773-82-1;Ertapenem;153832-46-3;Ertapenem-d4 disodium;1356934-56-9
|
| PubChem CID |
150611
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| Boiling Point |
813.9ºC at 760 mmHg
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| Melting Point |
230-234ºC
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| Flash Point |
446ºC
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| Vapour Pressure |
5.26E-28mmHg at 25°C
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| LogP |
0.39
|
| tPSA |
190.72
|
| SMILES |
C[C@@H]1[C@@H]2[C@@H]([C@@H](C)O)C(=O)N2C(=C1S[C@H]3C[C@@H](C(=NC4=CC=CC(=C4)C(=O)[O-])[O-])NC3)C(=O)O.[Na+].[Na+]
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| InChi Key |
KMVRATCHVMUJHM-SHZCTIMHSA-L
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| InChi Code |
InChI=1S/C22H25N3O7S.2Na/c1-9-16-15(10(2)26)20(28)25(16)17(22(31)32)18(9)33-13-7-14(23-8-13)19(27)24-12-5-3-4-11(6-12)21(29)30;;/h3-6,9-10,13-16,23,26H,7-8H2,1-2H3,(H,24,27)(H,29,30)(H,31,32);;/q;2*+1/p-2/t9-,10-,13+,14+,15-,16-;;/m1../s1
|
| Chemical Name |
disodium;(4R,5S,6S)-3-[(3S,5S)-5-[(3-carboxylatophenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
|
| Synonyms |
Ertapenem disodium; 153832-38-3; Ertapenem sodium; Ertapenem Disodium 90%; P5HEA33D9R; disodium;(4R,5S,6S)-3-[(3S,5S)-5-[(3-carboxylatophenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate; 153773-82-1; UNII-P5HEA33D9R;
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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 | 1.9250 mL | 9.6250 mL | 19.2500 mL | |
| 5 mM | 0.3850 mL | 1.9250 mL | 3.8500 mL | |
| 10 mM | 0.1925 mL | 0.9625 mL | 1.9250 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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