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Ertapenem (sodium salt)

Catalog No.
C3451
long-acting, broad-spectrum antibiotic
Grouped product items
SizePriceStock Qty
5mg
$79.00
In stock
10mg
$135.00
In stock
25mg
$281.00
In stock

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Email: [email protected]

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Background

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 [1].

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 [1]. 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 [2].

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 [3].

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.

References:
[1].  Shah P M, Isaacs R D. Ertapenem, the first of a new group of carbapenems[J]. Journal of antimicrobial Chemotherapy, 2003, 52(4): 538-542.
[2].  Wexler H M. In vitro activity of ertapenem: review of recent studies[J]. Journal of Antimicrobial Chemotherapy, 2004, 53(suppl 2): ii11-ii21.
[3].  Majumdar A K, Musson D G, Birk K L, et al. Pharmacokinetics of ertapenem in healthy young volunteers[J]. Antimicrobial Agents and Chemotherapy, 2002, 46(11): 3506-3511.

Chemical Properties

StorageStore at -20°C
M.Wt519.5
Cas No.153832-38-3
FormulaC22H23N3O7S·2Na
SynonymsL-749
Solubility≥52 mg/mL in H2O; insoluble in EtOH; ≥5.63 mg/mL in DMSO with ultrasonic
Chemical Name(4R,5S,6S)-3-[[(3S,5S)-5-[[(3-carboxyphenyl)amino]carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, disodium salt
SDFDownload SDF
Canonical SMILESO=C1[[email protected]@]([[email protected]@H](C)O)([H])[[email protected]]2([H])N1C(C([O-])=O)=C(S[[email protected]@H]3CN[[email protected]](C(NC4=CC(C([O-])=O)=CC=C4)=O)C3)[[email protected]@H]2C.[Na+].[Na+]
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

Penicillin-resistant S. pneumoniae

Preparation method

The solubility of this compound in H2O is ≥52mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

between 1 and 2 mg/L

Applications

It is worth noting that Ertapenem has a MIC90 value of 1 mg / L for many organisms, including Gram-positive cocci. In some studies, the MIC90 was slightly different (between 1 and 2 mg / L) in some species (such as penicillin-resistant S. pneumoniae).

Animal experiment [1]:

Animal models

Healthy young adults

Dosage form

3g, infusion

Application

In healthy young male and female volunteers, the average concentration of ertapenem in plasma after 30 minutes of infusion was from ~145 to 175 μg / ml, from~30 to 34 μg / ml at 6 h, and from ~ 9 to 11 μg / ml at 12 h. To. The mean t1 / 2 of plasma ranges from 3.8 to 4.4 hours. About 45% of the plasma clearance (CLP) comes from renal clearance.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wexler HM. In vitro activity of ertapenem: review of recent studies. J Antimicrob Chemother. 2004 Jun;53 Suppl 2: ii11-21. Review. PubMed PMID: 15150179.

[2]. Majumdar AK, Musson DG, Birk KL, Kitchen CJ, Holland S, McCrea J, Mistry G, Hesney M, Xi L, Li SX, Haesen R, Blum RA, Lins RL, Greenberg H, Waldman S, Deutsch P, Rogers JD. Pharmacokinetics of ertapenem in healthy young volunteers. Antimicrob Agents Chemother. 2002 Nov;46(11):3506-11. PubMed PMID: 12384357; PubMed Central PMCID: PMC128708.

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