C3451-25mg | Ertapenem (sodium salt) [153832-38-3] Clinisciences

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

Storage	Store at -20°C
M.Wt	519.5
Cas No.	153832-38-3
Formula	C₂₂H₂₃N₃O₇S·2Na
Synonyms	L-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
SDF	Download SDF
Canonical SMILES	O=C1[C@@]([C@@H](C)O)(10)[C@]2(10)N1C(C([O-])=O)=C(S[C@@H]3CN[C@H](C(NC4=CC(C([O-])=O)=CC=C4)=O)C3)[C@@H]2C.[Na+].[Na+]
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

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.

Quality Control

Purity = 98.10%

Chemical structure

Ertapenem (sodium salt) [153832-38-3]

Référence C3451-25mg

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