Polymyxin B (sulfate)
(Synonyms: 硫酸多粘菌素 B) 目录号 : GC15289A cationic peptide antibiotic,≥6000 U/mg
Cas No.:1405-20-5
Sample solution is provided at 25 µL, 10mM.
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].
多粘菌素B是由多粘菌属菌株产生的多肽混合物,包括多粘菌B1和B2。多粘菌素B对主要的多重耐药革兰阴性细菌、大多数真菌和革兰阳性细菌具有杀菌作用。作为由约八个氨基酸组成的碱性多肽,多粘菌素B具有对细胞膜的阳离子表面活性剂作用。此外,多粘菌素B可用于治疗由易感性铜绿假单胞菌菌株引起的脑膜炎、泌尿道感染和血液感染等革兰阴性菌感染。
体外:多粘菌素B可诱导树突状细胞成熟标志物的上调,包括共刺激分子CD86和HLA-I和II分子的表达增加。多粘菌素B可逐渐增强人类树突状细胞的粘附性质,并激活ERK1/2途径和IκB-α/NF-κB途径[1]。
体内:雄性败血症ddY小鼠皮下注射多粘菌素B,剂量为5、10、15或20 mg/kg,治疗7天。多粘菌素B以剂量依赖的方式改善了OU-01062和OU-98039感染小鼠的生存率。在多粘菌素B治疗的小鼠中,除了5 mg/kg的多粘菌素B外,每个浓度组的活细胞计数均趋于稳步降低。感染后3到6小时内细菌细胞数显著下降[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.
Cas No. | 1405-20-5 | SDF | |
别名 | 硫酸多粘菌素 B | ||
化学名 | N-(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 | ||
Canonical SMILES | O=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 | ||
分子式 | C56H98N16O13 • H2SO4 | 分子量 | 1301.6 |
溶解度 | H2O : ≥ 25 mg/mL | 储存条件 | Store at 2-8°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.7683 mL | 3.8414 mL | 7.6829 mL |
5 mM | 0.1537 mL | 0.7683 mL | 1.5366 mL |
10 mM | 0.0768 mL | 0.3841 mL | 0.7683 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Biological Activity: 7837U/mg
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet