Ertapenem (sodium salt)

Ertapenem, the first group of carbapenems, is a 1-β-methyl carbapenem with potent in vitro activity against a broad spectrum of bacterial pathogens including Gram-positive and Gram-negative aerobic and anaerobic pathogens . In vitro: In E.coli, ertapenem binds to penicillin binding proteins (PBPs) 1a, 1b, 2, 3, 4 and 5, showing highest affinity for PBPs 2 and 3 . MIC90s for most species of Enterobacteriaceae were < 1 mg/L. MIC90s for most Bacteroides fragilis group isolates ranged from 1 to 4 mg/L, and MIC90s were species specific for Clostridium, ranging from 0.06 mg/L for Clostridium perfringens to 4 mg/L for Clostridiumclostridioforme . In vivo: In healthy young men and women volunteers, the mean concentration of ertapenem in plasma ranged from ~145 to 175 μg/ml at the end of a 30-min infusion, from ~30 to 34 μg/ml at 6 h, and from ~9 to 11 μg/ml at 12 h. The mean plasma t1/2 ranged from 3.8 to 4.4 h. About 45% of the plasma clearance (CLP) was via renal clearance . Clinical trials: Ertapenem was highly effective in patients with a range of disease severity within each indication, including elderly patients and patients with severe infections. Ertapenem is not hepatically metabolized and is primarily eliminated by the renal route; dose reduction to 0.5 g once a day is required in patients with severe renal insufficiency. Ertapenem is rapidly bactericidal. The most common adverse reactions reported with ertapenem were diarrhoea, nausea, infused vein complication, vaginitis, headache in females, phlebitis/thrombophlebitis, vomiting and elevated aminotransferase levels.

Product information

CAS Number: 153832-38-3

Molecular Weight: 519.48

Formula: C22H23N3Na2O7S

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

Smiles: [Na+].[Na+].C[C@@H]1[C@@H]2[C@@H]([C@@H](C)O)C(=O)N2C(=C1S[C@@H]1CN[C@@H](C1)C(=O)NC1C=CC=C(C=1)C([O-])=O)C([O-])=O

InChiKey: KMVRATCHVMUJHM-SHZCTIMHSA-L

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.