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4135-11-9

中文名稱 polymyxin B(1)
英文名稱 polymyxin B(1)
CAS 4135-11-9
分子式 C56H98N16O13
分子量 1203.48
MOL 文件 4135-11-9.mol
更新日期 2024/12/15 17:53:36
4135-11-9 結(jié)構(gòu)式 4135-11-9 結(jié)構(gòu)式

基本信息

中文別名
多粘菌素B1
多黏菌素 B1
多粘菌素B1 POLYMYXIN B1
英文別名
polymyxin B(1)
(-)-N2-[[(6S)-6-Methyloctanoyl]-L-A2bu-L-Thr-L-A2bu-]cyclo(L-A2bu*-L-A2bu-D-Phe-L-Leu-L-A2bu-L-A2bu-L-Thr-)
(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-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methyloctanamide

物理化學(xué)性質(zhì)

沸點(diǎn)838.79°C (rough estimate)
密度1.0500 (rough estimate)
折射率1.6200 (estimate)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度PBS (pH 7.2): 2 mg/ml
酸度系數(shù)(pKa)13.08±0.70(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

常見問題列表

生物活性
Polymyxin B1 是一種有效的抗菌脂肽,衍生自多頭芽孢桿菌。Polymyxin B1 是 Polymyxin B (HY-A0248) 的主要成分。Polymyxin B1 可以通過與細(xì)菌細(xì)胞膜的相互作用來誘導(dǎo)細(xì)菌細(xì)胞裂解。Polymyxin B1 可用于多重耐藥性革蘭氏陰性菌感染的研究。
體外研究

Polymyxin B1 has antimicrobial activity that againsts Pseudomonas aeruginosa ATCC 27853, Acinetobacter baumannii ATCC BAA 747, Klebsiella pneumoniae ATCC 13883, P. aeruginosa 9019, A. baumannii 1261 and K. pneumoniae VM9 isolates with MIC values of 4 μg/mL, 2 μg/mL, 2 μg/mL, 4 μg/mL, 4 μg/mL and 2 μg/mL, respectively.
Polymyxin B1 strongly inhibits protein synthesis in yeast, and in E. coli and S. aureus .

體內(nèi)研究

The pharmacokinetics of Polymyxin B1 is investigated in a rat model following intravenous administration (0.8 mg/kg). The area under the concentration-time curve for Polymyxins B1 is greater than those of colistins A and B. Colistin A colistin B. The clearance value of Polymyxins B1 is 2.39 mL/min/kg, the plasma protein binding is 82.3%, the elimination half-life is 79.5 min and the AUC 0-∞ is 365 mg?min/L.

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