64221-86-9

• 常用中文名：亚胺培南
• 常用英文名：Imipenem
• CAS号：64221-86-9
• 分子式：C₁₂H₁₉N₃O₅S
• 分子量：299.346
• 相关类别： 原料药 抗生素类药物 β-内酰胺酶抑制剂
• 发布时间：2018-07-09 16:35:17
• 更新时间：2024-01-05 20:03:33
• 亚胺培南(N-甲酰胺基噻霉素,MK0787)是噻霉霉素的稳定结晶衍生物,是一种抗生素,对广泛的革兰氏阳性菌和革兰氏阴性需氧菌和厌氧菌具有优异的活性。亚胺培南(N-甲酰噻霉素,MK0787)可用于碳青霉烯不敏感和铜绿假单胞菌生物膜感染[1][2][3]。

名称

• 中文名: 亚胺培南
• 英文名: imipenem
• 中文别名: 6-(1-羟基乙基)-3-[[2-[(亚氨基甲基)氨基]乙基]硫]-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-甲酸; 亚安培南; (5R,6S)-6-[(1R)-1-羟乙基]-3-[[2-[(亚氨基甲基)氨基]乙基]硫代]-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸单水合物
• 英文别名: N-Formimidoylthienamycin; LMipeneM; imipenam; (5R,6S)-6-[(1R)-1-hydroxyethyl]-3-({2-[(iminomethyl)amino]ethyl}thio)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid; (5R,6S)-6-[(1R)-1-Hydroxyethyl]-3-({2-[(iminomethyl)amino]ethyl}sulfanyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid; EINECS 264-734-5; (5R,6S)-6-(1-hydroxyethyl)-3-({2-[(iminiomethyl)amino]ethyl}sulfanyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate; (5R,6S)-3-((2-(Formimidoylamino)ethyl)thio)-6-((R)-1-hydroxyethyl)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid; 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 6-(1-hydroxyethyl)-3-[[2-[(iminomethyl)amino]ethyl]thio]-7-oxo-, (5R,6S)-; 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 6-[(1R)-1-hydroxyethyl]-3-[[2-[(iminomethyl)amino]ethyl]thio]-7-oxo-, (5R,6S)-; Tienamycin; imipemide; N-Formimidoylthiena; (5R,6S)-6-((R)-1-Hydroxyethyl)-3-(2-(iminomethylamino)ethylthio)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carbonsaeure; Imipenem (JP14); Imipenen; mk-787; Imipenem; MFCD00864955

物化性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 530.2±60.0 °C at 760 mmHg
• 熔点: 106-111ºC
• 分子式: C₁₂H₁₉N₃O₅S
• 分子量: 299.346
• 闪点: 274.5±32.9 °C
• 精确质量: 299.093964
• PSA: 148.25000
• LogP: -2.78
• 外观性状: 白色结晶粉末
• 蒸汽压: 0.0±3.2 mmHg at 25°C
• 折射率: 1.721

生物活性

• 描述: 亚胺培南(N-甲酰胺基噻霉素,MK0787)是噻霉霉素的稳定结晶衍生物,是一种抗生素,对广泛的革兰氏阳性菌和革兰氏阴性需氧菌和厌氧菌具有优异的活性。亚胺培南(N-甲酰噻霉素,MK0787)可用于碳青霉烯不敏感和铜绿假单胞菌生物膜感染[1][2][3]。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 参考文献:

  [1]. Johann Motsch, et al. RESTORE-IMI 1: A Multicenter, Randomized, Double-blind Trial Comparing Efficacy and Safety of Imipenem/Relebactam vs Colistin Plus Imipenem in Patients With Imipenem-nonsusceptible Bacterial Infections. Clin Infect Dis. 2020 Apr 15;70(9):1799-1808.

  [2]. F P Tally, et al. In vitro activity of N-formimidoyl thienamycin (MK0787). Antimicrob Agents Chemother. 1980 Oct;18(4):642-4.

  [3]. Wang Hengzhuang, et al. In vivo pharmacokinetics/pharmacodynamics of colistin and imipenem in Pseudomonas aeruginosa biofilm infection. Antimicrob Agents Chemother. 2012 May;56(5):2683-90.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CL5446520 CHEMICAL NAME : 1-Azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid, 6-(1-hydroxyethyl)-3-((2-((iminomethyl) amino)ethyl)thio)-7-oxo-, (5R-(5-alpha,6-alpha(R*)))- CAS REGISTRY NUMBER : 64221-86-9 LAST UPDATED : 199409 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C12-H17-N3-O4-S MOLECULAR WEIGHT : 299.38 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1972 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1660 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 664 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 45,1983,1992

安全

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): R36/37/38
• 安全声明 (欧洲): 26-27-36/37/39
• 海关编码: 29419000

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