您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Polymyxin B1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Polymyxin B1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Polymyxin B1图片
CAS NO:4135-11-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
多粘菌素 B1 是一种强效抗菌脂肽,最初来源于多粘芽孢杆菌。
Cas No.4135-11-9
别名多粘菌素 B1
化学名(S)-N-((S)-4-amino-1-(((2S,3R)-1-(((S)-4-amino-1-oxo-1-(((3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-((R)-1-hydroxyethyl)-12-isobutyl-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl)amino)butan-2-yl)a
Canonical SMILESO=C([C@@H](NC([C@H](CCN)NC(CCCC[C@@H](C)CC)=O)=O)[C@@H](C)O)N[C@@H](CCN)C(N[C@@H](CCNC([C@@H](NC([C@@H](NC([C@H](CCN)N1)=O)CCN)=O)[C@H](O)C)=O)C(N[C@@H](CCN)C(N[C@H](CC2=CC=CC=C2)C(N[C@@H](CC(C)C)C1=O)=O)=O)=O)=O
分子式C56H98N16O13
分子量1203.5
溶解度2 mg/ml in PBS (pH 7.2)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Polymyxin B1 can bind and kill Gram-negative bacteria.

In view of the emergence of multidrug resistance among Gram-negative bacteria, polymyxin B has emerged as one of the therapeutic agents of last resort.

In vitro: Previous study reported the first molecular dynamics simulation investigation of the interaction of polymyxin B1 with complex models of membranes of E. coli. The results of >16 microseconds of simulation predicted that polymyxin B1 was probably to interact with the membranes via distinct mechanisms. Polymyxin B1 aggregated in the lipopolysaccharide headgroup region of the outer membrane with limited tendency for insertion within the lipid A tails. Whereas, polymyxin B1 readily insert into the inner membrane core, and the concomitant increased hydration might be responsible for bilayer destabilization and antimicrobial function [1].

In vivo: The PK parameters of the major components including polymyxin B1 from Polymyxin B did not appear to be significantly different. Less than 1% of the dose was recovered unchanged in urine collected over 48 h. Therapeutic drug concentrations maintained in kidney tissue at 48 h. The post-renal insufficiency to pre-renal insufficiency ratio of the area under the serum concentration-time curve from time zero to infinity was 1.33. Polymyxin B components seemed to have similar pharmacokinetics. Polymyxin B preferentially persisted in kidneys, suggesting a selective uptake process in renal cells [2].

Clinical trial: Treatment of patients with PMB1 has been shown to have adverse side effects on the renal and nervous system, and thus clinical use of PMB1 has been limited to topical treatment and “last resort” therapy of patients infected with multidrug-resistant bacteria or with chronic conditions who suffer from recurring respiratory infections [1].

References:
[1] Nils A. Berglund, Thomas J. Piggot, Damien Jefferies, Richard B. Sessions, Peter J. Bond, Syma Khalid. Interaction of the Antimicrobial Peptide Polymyxin B1 with Both Membranes of E. coli: A Molecular Dynamics Study. PLoS Comput Biol. 2015 Apr; 11(4): e1004180.
[2] Kamilia Abdelraouf, Jie He, Kimberly R. Ledesma, Ming Hu, and Vincent H. Tam. Pharmacokinetics and Renal Disposition of Polymyxin B in an Animal Model. Antimicrob Agents Chemother. 2012 Nov; 56(11): 5724–5727.