4135-11-9

• 常用中文名：Polymyxin B1
• 常用英文名：Polymyxin B1
• CAS号：4135-11-9
• 分子式：C₅₆H₉₈N₁₆O₁₃
• 分子量：1203.477
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2017-12-18 03:36:38
• 更新时间：2024-01-04 18:58:14
• Polymyxin B1 是一种有效的抗菌脂肽,衍生自多头芽孢杆菌。Polymyxin B1 是 Polymyxin B (HY-A0248) 的主要成分。Polymyxin B1 可以通过与细菌细胞膜的相互作用来诱导细菌细胞裂解。Polymyxin B1 可用于多重耐药性革兰氏阴性菌感染的研究。

名称

• 中文名: 多粘菌素B1硫酸盐
• 英文名: polymyxin B1
• 英文别名: (6S)-N-[(2S)-4-Amino-1-{[(2S,3R)-1-{[(2S)-4-amino-1-oxo-1-({(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-isobutyl-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl}amino)-2-butanyl]amino}-3-hydroxy-1-oxo-2-butanyl]amino}-1-oxo-2-butanyl]-6-methyloctanamide; polymyxin B; Octanamide, N-[(1S)-3-amino-1-[[[(1S,2R)-1-[[[(1S)-3-amino-1-[[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-15-(phenylmethyl)-1,4,7,10,13,16,19-heptaazacyclotricos-21-yl]amino]carbonyl]propyl]amino]carbonyl]-2-hydroxypropyl]amino]carbonyl]propyl]-6-methyl-, (6S)-; Polymyxin B1; polymixin B1

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 1571.6±65.0 °C at 760 mmHg
• 分子式: C₅₆H₉₈N₁₆O₁₃
• 分子量: 1203.477
• 闪点: 904.2±34.3 °C
• 精确质量: 1202.749878
• PSA: 490.66000
• LogP: -2.87
• 蒸汽压: 0.0±0.3 mmHg at 25°C
• 折射率: 1.592
• 储存条件: -20°C， 充氩

生物活性

• 描述: Polymyxin B1 是一种有效的抗菌脂肽,衍生自多头芽孢杆菌。Polymyxin B1 是 Polymyxin B (HY-A0248) 的主要成分。Polymyxin B1 可以通过与细菌细胞膜的相互作用来诱导细菌细胞裂解。Polymyxin B1 可用于多重耐药性革兰氏阴性菌感染的研究。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 体外研究: 多粘菌素B1对铜绿假单胞菌ATCC 27853、鲍曼不动杆菌ATCC BAA 747、肺炎克雷伯菌ATCC 13883、铜绿假单胞菌9019、鲍曼假单胞菌1261和肺炎克雷伯菌VM9的MIC值分别为4μg/mL、2μg/mL、2μg/mL、4μg/mL、4μg/mL和2μg/mL具有抗菌活性[3]。多粘菌素B1强烈抑制酵母、大肠杆菌和金黄色葡萄球菌中的蛋白质合成[4]。
• 体内研究: 多粘菌素B1在大鼠静脉注射(0.8mg/kg)后的药代动力学研究。多粘菌素B1的浓度-时间曲线下面积大于粘菌素A和粘菌素B,多粘菌素B1的清除率为2.39ml/min/kg,血浆蛋白结合率为82.3%,清除半衰期为79.5min,AUC0-∞为365mg•min/L[5]。
• 参考文献:

  [1]. Kwa AL, et al. Pharmacokinetics of polymyxin B1 in patients with multidrug-resistant Gram-negative bacterial infections. Diagn Microbiol Infect Dis. 2008 Feb;60(2):163-7.

  [2]. Berglund NA, et al. Interaction of the antimicrobial peptide polymyxin B1 with both membranes of E. coli: a molecular dynamics study. PLoS Comput Biol. 2015 Apr 17;11(4):e1004180.

  [3]. Tam VH, et al. In vitro potency of various polymyxin B components. Antimicrob Agents Chemother. 2011 Sep;55(9):4490-1.

  [4]. Alonso MA, et al. Compounds affecting membranes that inhibit protein synthesis in yeast. Antimicrob Agents Chemother. 1979 Dec;16(6):750-6.

  [5]. Sivanesan S, et al. Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats. J Nat Prod. 2017 Jan 27;80(1):225-229.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TR1055000 CHEMICAL NAME : Polymyxin B1 CAS REGISTRY NUMBER : 4135-11-9 LAST UPDATED : 199612 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C56-H98-N16-O13 MOLECULAR WEIGHT : 1203.70 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 19 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 80 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1500 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980

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