Ertapenem sodium

SKU: orb1221314

Description

Ertapenem sodium is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.(In Vitro):Ertapenem sodium (0-100 μg/mL approximately, 48 h) is active against 99.1% of all anaerobes with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL, and MIC’s ≥8 μg/mL for B.fragilis and B.vulgatus species, respectively.(In Vivo):Ertapenem sodium (Subcutaneous injection, 0-10 mg/kg, 0-120 h after infection, S. aureus thigh tissue infection model) shows > 3 log10 CFU reduction of organism at 10 mg/kg, and maintains the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg.Ertapenem sodium (Subcutaneous injection, 4h after infection, systemic infection model) is active against all gram-positive organisms, and is also active against gram-negative organisms tested with ED50s of <0.25 mg/kg/dose.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 153773-82-1
• MW: 497.502
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₄N₃O₇S.Na
• SMILES: [Na+].C[C@@H](O)[C@@H]1[C@H]2[C@@H](C)C(S[C@@H]3CN[C@@H](C3)C(=O)Nc3cccc(c3)C([O-])=O)=C(N2C1=O)C(O)=O
• Target: Antibiotic
• Solubility: DMSO:201 mM;water:100.5mM

Bioactivity

• In Vivo:
  Ertapenem sodium (Subcutaneous injection, 0-10 mg/kg, 0-120 h after infection, S. aureus thigh tissue infection model) shows > 3 log10 CFU reduction of organism at 10 mg/kg, and maintains the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg. Ertapenem sodium (Subcutaneous injection, 4h after infection, systemic infection model) is active against all gram-positive organisms, and is also active against gram-negative organisms tested with ED50s of <0.25 mg/kg/dose. Animal model: S. aureus thigh tissue infection model (DBA/2 mice). 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: 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 model: Systemic infection model (DBA/2 female mice, viral antibody-free CD-1 female mice). Dosage: 0-3 mg/kg approximately. Administration: Subcutaneous injection (0.5 mL, begin immediately and 4 h after infection). Result: Showed activity against all gram-positive organisms, and also ram-negative organisms tested with ED50s of <0.25 mg/kg/dose. Animal model: CD-1 mice, rats. Dosage: 10 mg/kg approximately. Administration: Intraperitoneal injection (pharmacokinetic assay). Result: Exhibited an AUC0-∞ ranging from 1.8-21.82 μg hr/mL in tissue in mice following a 10-mg/kg i.p. dose. Exhibited slow clearance rate with a t1/2β of 3.2 h, Clp of 0.47 mL/min/kg, AUC0-8 of 284.15 μg hr/mL.
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• In Vitro:
  Ertapenem sodium (0-100 μg/mL approximately, 48 h) is active against 99.1% of all anaerobes with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL, and MIC’s ≥8 μg/mL for B. fragilis and B. vulgatus species, respectively. Cell Viability 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: 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MK-826 | L-749345

Quick Database Links

Gene Symbol

Antibiotic