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Colistin sulfate (Belcomycin; Polymixin E), originally isolated from B. polymyxa, is a polypeptide antibiotic and apoptosis inducer, also acts as a NADH quinone oxidoreductase inhibitor. It inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
| ln Vitro |
Colistins work like detergents to kill gram-negative bacteria. This mechanism includes competitively displacing divalent cations (calcium and magnesium) from the negatively charged phosphate groups of membrane lipids, as well as interaction with the lipopolysaccharides and phospholipids of the outer membrane through electrostatic interference[1]. Colistin, also known as polymyxin E, is a good treatment for infections brought on by gram-negative bacteria that are resistant to many drugs because of its quick bacterial killing, limited spectrum of action, and concomitant delayed development of resistance. Commercially, colistin comes in two forms: colistin methanesulfonate (sodium) for parenteral use and colistin (sulfate), primarily for topical use[2].
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| ln Vivo |
Following intraperitoneal instillation, slow and sustained CMS conversion leads to high concentrations of colistin in rat ELF[3]. Piglets are frequently given colonistin, however both under- and overdosing are common. The fecal microbiota of piglets is not significantly disrupted by colistin overdoses or underdoses, and chromosomal resistance in the predominant E. coli population is seldom selected for[4].
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| Animal Protocol |
Rats: Sterile 0.9% sodium chloride is used to prepare fresh dose solutions of colistin methanesulfonate (sodium) and colistin sulfate. Colistin methanesulfonate (CMS) or sulfate solutions are injected bolus-xstyle through the jugular vein cannula for the intravenous studies. The method for pulmonary administration is called intratracheal (i.t.) instillation. CMS is given intravenously to animals at doses of 14 mg/kg, 28 mg/kg, or 56 mg/kg of body weight. Colistin is given intraperitoneally (i.v.) to rats in an independent study at doses of 0.21 mg/kg, 0.41 mg/kg, or 0.62 mg/kg[3].
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| References |
| Molecular Formula |
C52H98N16O13.2.5H2O4S
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|---|---|
| Molecular Weight |
1400.64
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| Exact Mass |
1,266.73
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| Elemental Analysis |
C, 50.22; H, 8.11; N, 17.68; O, 21.46; S, 2.53
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| CAS # |
1264-72-8
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| Related CAS # |
Colistin;1066-17-7
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| Appearance |
Solid powder
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| SMILES |
O=C(N[C@@H](CCN)C(N[C@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCN)C(N[C@H]1CCN)=O)=O)=O)=O)[C@@H](NC([C@H](CCN)NC([C@@H](NC([C@H](CCN)NC(CCCC[C@H](C)CC)=O)=O)[C@@H](C)O)=O)=O)CCNC([C@H]([C@@H](C)O)NC1=O)=O.OS(O)(=O)=O
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| InChi Key |
ZJIWRHLZXQPFAD-FPSDIOKYSA-N
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| Chemical Name |
(R)-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)-3-((R)-1-hydroxyethyl)-12,15-diisobutyl-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-yl)-6-methyloctanamide sulfate
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| Synonyms |
Belcomycin; Polymixin E; Colistin sulfate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~35.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (35.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7140 mL | 3.5698 mL | 7.1396 mL | |
| 5 mM | 0.1428 mL | 0.7140 mL | 1.4279 mL | |
| 10 mM | 0.0714 mL | 0.3570 mL | 0.7140 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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