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Polymyxin B (sulfate)

硫酸多粘菌素 B
Catalog No.
C3090
具有杀菌活性,针对主要的多药耐药性革兰氏阴性细菌
组合的产品项目
规格价格库存 数量
1g
¥ 626.00
Ship with 10-15 days
5g
¥ 2,068.00
Ship with 10-15 days

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背景

Polymyxin B, a mixture of polymyxins B1 and B2, is obtained from Bacillus polymyxa strains. Polymyxin B exhibits bactericidal activity against major multidrug-resistant gram-negative bacteria, most fungi and gram-positive bacteria. As basic polypeptides of about eight amino acids, polymyxins B1 and B2 have cationic detergent action on cell membranes. Moreover, polymyxin B is used for infections with gram-negative organisms, which may be nephrotoxic and neurotoxic. Polymyxin B is appropriate to treat the infections of the meninges, urinary tract, and blood stream, triggered by susceptible Pseudomonas aeruginosa strains.

In vitro: Polymyxin B elicited up-regulation of dendritic cells (DCs) maturation markers, including the increase in the in the expression of co-stimulatory molecule CD86 and HLA-class I and II molecules. Polymyxin B induced a progressive increase in the adhesion property of human DCs. In addition, polymyxin B triggered the activation of the ERK1/2 pathway and IκB-α/NF-κB pathways [1].

In vivo: Male bacteraemia ddY mice were subcutaneously treated with polymyxin B at a dose of 5, 10, 15 or 20 mg/kg for 7 days. Polymyxin B, in a dose-dependent fashion, improved the survival both of OU-01062- and OU-98039-infected mice. In polymyxin B-treated mice, except for 5 mg/kg polymyxin B, the viable cell counts had a tendency to reduce steadily in each concentration group. It was showed a rapid and marked decline of bacterial cell count between 3 to 6 h after infection [2].

References:
[1].  Valentinis, B., Bianchi, A., Zhou, D., Cipponi, A., Catalanotti, F., Russo, V., & Traversari, C. Direct Effects of Polymyxin B on Human Dendritic Cells Maturation: THE ROLE OF I B- /NF- B AND ERK1/2 PATHWAYS AND ADHESION. Journal of Biological Chemistry. 2005; 280(14): 14264-14271.
[2].  Miyajima, Y., Hiramatsu, K., Mizukami, E., Morinaga, R., Ishii, H., & Shirai, R. et al. In vitro and in vivo potency of polymyxin B against IMP-type metallo-β-lactamase-producing Pseudomonas aeruginosa. International Journal of Antimicrobial Agents. 2008; 32(5): 437-440.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt1301.6
Cas No.1405-20-5
FormulaC56H98N16O13·H2SO4
SynonymsAerosporin,Mastimyxin
Solubility≤2mg/ml in PBS(pH7.2)
Chemical NameN-(4-amino-1-((1-((4-amino-1-oxo-1-((6,9,18-tris(2-aminoethyl)-15-benzyl-3-(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)amino)-3-hydroxy-1-oxobutan-2-yl)amino)-1-oxobutan-2
SDFDownload SDF
Canonical SMILESO=C(C(NC(C(CCN)NC(CCCCC(C)CC)=O)=O)C(C)O)NC(CCN)C(NC(CCNC(C(NC(C(NC(C(CCN)N1)=O)CCN)=O)C(O)C)=O)C(NC(CCN)C(NC(CC2=CC=CC=C2)C(NC(CC(C)C)C1=O)=O)=O)=O)=O.O=S(O)(O)=O
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化学结构

Polymyxin B (sulfate)