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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEColistin sulfateCat. No.: HY-A0089CAS No.: 1264-72-8Synonyms: Polymyxin E Sulfate分式: CHNOS分量: 1253.51作靶点: Bacterial; Autophagy作通路: Anti-infection; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解
2、性数据体外实验 H2O : 32 mg/mL (25.53 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.7978 mL 3.9888 mL 7.9776 mL5 mM 0.1596 mL 0.7978 mL 1.5955 mL10 mM 0.0798 mL 0.3989 mL 0.7978 mL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,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Colistin种多肽
3、抗素,其通过与兰性细的外细胞膜中的脂多糖和磷脂结合来抑制兰性细体外研究Colistins are bactericidal to gram-negative bacteria by a detergent-like mechanism. This mechanism involvesinteraction with lipopolysaccharides and phospholipids of the outer membrane and electrostatic interference1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEwi
4、th the outer membrane by competitively displacing divalent cations (calcium and magnesium) from thenegatively charged phosphate groups of membrane lipids 1. Colistin (polymyxin E) owns favorableproperties of rapid bacterial killing, a narrow spectrum of activity, and an associated slow development o
5、fresistance for the treatment of infections caused by multidrug-resistant gram-negative bacteria. There aretwo forms of colistin available commercially: colistin (sulfate) mainly for topical use and colistinmethanesulfonate (sodium) for parenteral use 2.体内研究 High concentrations of colistin in rat EL
6、F are achieved as a result of slow and sustained CMS conversionfollowing i.t. instillation 3. Colistin is often used in piglets but underdosing and overdosing are frequent.Under- or overdoses of colistin do not result in any major disturbance of piglet fecal microbiota and rarelyselect for chromosom
7、al resistance in the dominant E. coli population 4.PROTOCOLAnimal Rats: Colistin methanesulfonate (sodium) and colistin (sulfate) dosing solutions are freshly prepared in sterileAdministration 3 0.9% sodium chloride. For the i.v. studies, colistin methanesulfonate (CMS) or sulfate solutions areadmin
8、istered by a bolus injection via the jugular vein cannula. Intratracheal (i.t.) instillation is utilized as thetechnique for pulmonary administration. Animals are administered i.v. CMS at doses of 14 mg/kg of bodyweight, 28 mg/kg or 56 mg/kg. In an independent study, rats are administered i.v. colis
9、tin at doses of 0.21mg/kg, 0.41 mg/kg, or 0.62 mg/kg 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only. J Antibiot (Tokyo). 2019 Apr 26.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hancock RE et al. Peptide antibiotics. Antimicr
10、ob Agents Chemother. 1999 Jun;43(6):1317-23.2. Li J, et al. In vitro pharmacodynamic properties of colistin and colistin methanesulfonate againstPseudomonas aeruginosa isolates frompatients with cystic fibrosis. Antimicrob Agents Chemother. 2001 Mar;45(3):781-5.3. W S Yapa S, et al. Population pharm
11、acokinetics of colistin methanesulfonate in rats: achieving sustained lung concentrations of colistinfor targeting respiratory infections. Antimicrob Agents Chemother. 2013 Oct;57(10):5087-95.4. Fleury MA, et al. Impact of two different colistin dosing strategies on healthy piglet fecal microbiota. Res Vet Sci. 2016 Aug;107:152-60.McePdfHeightCaution: Product has no
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