Ertapenem(sodium salt)

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CAS NO:

153832-38-3

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

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
Canonical SMILES	O=C1[C@@]([C@@H](C)O)([H])[C@]2([H])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+]
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

细胞实验 [1]：
细胞系	耐青霉素的肺炎链球菌
溶解方法	在H₂O中的溶解度≥52mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。
反应条件	1 ~ 2 mg/L
应用	值得注意的是，对于许多生物（包括革兰氏阳性球菌），Ertapenem的MIC90值为1 mg / L。在某些研究中，某些物种（例如耐青霉素的肺炎链球菌）的MIC90略有不同（介于1和2 mg / L之间）。
动物实验 [2]：
动物模型	健康的年轻人
剂量	3g，输注
应用	在健康的年轻男性和女性志愿者中，输注30分钟后血浆中ertapenem的平均浓度范围为约为145至175μg/ ml，在6 h时约为30至34μg/ ml，在12 h约为9至11μg/ ml。血浆的平均t1 / 2范围为3.8至4.4小时。约45%的血浆清除率（CLP）来自肾脏清除。
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。
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.