4135-11-9
4135-11-9 结构式
基本信息
多黏菌素 B1
多粘菌素B1 POLYMYXIN B1
(-)-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
物理化学性质
常见问题列表
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
.
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.