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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Ertapenem sodium (MK-0826; L-749345; Invanoz; Invanz), the sodium salt of ertapenem, is a 1-β-methyl carbapenem antibiotic marketed by Merck as Invanz. Ertapenem is a long-acting, broad-spectrum antibiotic of β-lactam subclass. Ertapenem has a broad spectrum of antibacterial activity including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases. Ertapenem is an inhibitor of bacteria cell-wall synthesis, it acts by binding to penicillin binding proteins 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. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases.
Targets |
β-lactam
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ln Vitro |
Ertapenem sodium (0-100 μg/mL, approximately 48 hours) exhibits activity against 99.1% of all anaerobes, with MICs for B.fragilis and B.vulgatus species being ≥8 μg/mL and 0.12 μg/mL and MIC90 of 1 μg/mL, respectively[1].
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ln Vivo |
In a S. aureus thigh tissue infection model, subcutaneous injection of ertapenem sodium (0–10 mg/kg, 0-120 h post-infection) reduces the organism by > 3 log10 CFU at 10 mg/kg and keeps the activity at 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg[2].
In addition to being active against all gram-positive organisms, ertapenem sodium (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 Line: B. fragilis (ATCC 25285), B. thetaiotaomicron (ATCC 29741), and Eubacterium lentum (ATCC 43055)
Concentration: 0-100 μg/mL approximately Incubation Time: 48 h Result: 98.8% of the isolates in the B. fragilis group were susceptible, and 99.1% of all isolates were inhibited with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL. |
Animal Protocol |
Animal Model: S. aureus thigh tissue infection model (DBA/2 mice)[2]
Dosage: 0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10, 24, 48, 72, 96, 120 h) Administration: Subcutaneous injection (0.5 mL after infection) Result:> 3 logs were displayed.10 CFU decrease in the organism when compared to controls not receiving antibiotics at a dose of 10 mg/kg. Maintained the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg. |
References | |
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 |
C22H24N3NAO7S
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Molecular Weight |
497.5
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Exact Mass |
474.13
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Elemental Analysis |
C, 53.11; H, 4.86; N, 8.45; Na, 4.62; O, 22.51; S, 6.45
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CAS # |
153773-82-1
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Related CAS # |
Ertapenem disodium;153832-38-3;Ertapenem;153832-46-3
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PubChem CID |
23674512
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Appearance |
White to light yellow solid powder
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Boiling Point |
813.9ºC at 760 mmHg
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Flash Point |
446ºC
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Vapour Pressure |
5.26E-28mmHg at 25°C
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tPSA |
184.4
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SMILES |
O=C([C@H]1NC[C@@H](SC2=C(C(O)=O)N3[C@]([C@]([C@@H](C)O)([H])C3=O)([H])[C@H]2C)C1)NC4=CC=CC(C([O-])=O)=C4.[Na+]
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InChi Key |
ZXNAQFZBWUNWJM-HRXMHBOMSA-M
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InChi Code |
InChI=1S/C22H25N3O7S.Na/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;+1/p-1/t9-,10-,13+,14+,15-,16-;/m1./s1
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Chemical Name |
Sodium;3-[[(2S,4S)-4-[[(4R,5S,6S)-2-carboxy-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]sulfanyl]pyrrolidine-2-carbonyl]amino]benzoate
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Synonyms |
MK 826; L-749345; MK-826; L749345; MK826; MK-0826; MK 0826; MK0826; L 749345; Ertapenem Sodium; Trade Name: Invanoz;Ertapenem sodium; 153773-82-1; ertapenem monosodium; Ertapenem sodium salt; UNII-2T90KE67L0; CHEBI:60070; Invanz (TN); Invanz
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
DMSO : ~100 mg/mL ( ~201.0 mM O)
Water : 50~100 mg/mL(~100.50 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (201.01 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0101 mL | 10.0503 mL | 20.1005 mL | |
5 mM | 0.4020 mL | 2.0101 mL | 4.0201 mL | |
10 mM | 0.2010 mL | 1.0050 mL | 2.0101 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.