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Colistin sulfate

Product Name
Colistin sulfate
CAS No.
1264-72-8
Chemical Name
Colistin sulfate
Synonyms
COLISTIN SULPHATE;POLYMYXIN E;COLISTINE SULFATE;CoL;COLISTIN SULFATE SALT;COLISTINE SULPHATE;belcomycin;Colomyci;istin suL;Belcomycine
CBNumber
CB8359485
Molecular Formula
2(C52H98N16O13).5(H2SO4)
Formula Weight
2801.27
MOL File
1264-72-8.mol
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Colistin sulfate Property

Melting point:
200-220°C
storage temp. 
Inert atmosphere,2-8°C
solubility 
H2O: soluble50mg/mL
form 
powder
PH
4.0~6.0(10g/l, 25℃)
Water Solubility 
Soluble in water
Merck 
14,2479
InChIKey
VEXVWZFRWNZWJX-NBKAJXASSA-N
CAS DataBase Reference
1264-72-8(CAS DataBase Reference)
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Safety

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1/PG 3
WGK Germany 
3
RTECS 
TR1500000
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
29419000
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
C4461
Product name
Colistin sulfate salt
Purity
≥15,000 U/mg
Packaging
1g
Price
$254
Updated
2024/03/01
Sigma-Aldrich
Product number
1148001
Product name
Colistin sulfate
Packaging
200mg
Price
$457
Updated
2024/03/01
Alfa Aesar
Product number
J67415
Product name
Colistin sulfate, 50 mg/ml in distilled water, sterile-filtered
Packaging
5x1ml
Price
$233.65
Updated
2024/03/01
Alfa Aesar
Product number
J60915
Product name
Colistin sulfate
Packaging
1g
Price
$169
Updated
2024/03/01
Cayman Chemical
Product number
17584
Product name
Colistin (sulfate)
Packaging
1g
Price
$33
Updated
2024/03/01
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Colistin sulfate Chemical Properties,Usage,Production

Chemical Properties

White or almost white, hygroscopic powder.

Uses

antibacterial

Uses

neuromuscular blocker

Uses

Cyclic polypeptide antibiotic produced by Bacillus polymyxa. Complex mixture of at least 30 components, primarily colistins A and B. [a]D= -65?(c= 1, Water) LOD: 3%

Uses

Colistin sulfate A Polymyxin potent antibiotic and apoptosis inducer. This compound induces apoptosis through interaction with the cytoplasmic membrane. Colistin is a key microbiological component in Colistin Oxolinic Acid Blood Agar utilized in the cultivation of Aminobacter aminovorans, Bacillus species, Hyphomicrobium species and Methylobacterium species. It is also a critical component is VCN Inhibitor & VCNT Inhibitor growth media used in the isolation of Neisseria species.

brand name

Coly-Mycin (Monarch).

Antimicrobial activity

All the polymyxins have a similar antibacterial spectrum, although there are slight quantitative differences in their activity in vitro. They are inactive against Gram-positive organisms, but nearly all enterobacteria, except Proteus spp., Burkholderia cepacia and Ser. marcescens, are highly susceptible. The MIC of polymyxin B or colistin sulfate for Esch. coli and Klebsiella spp. is 0.01–1 mg/L; the corresponding concentration for Ps. aeruginosa is 0.03–4 mg/L. Bacteroides fragilis is resistant, but other Bacteroides spp. and fusobacteria are susceptible. Resistance of V. cholerae eltor to polymyxin B distinguishes it from the classic vibrio.
The sulfomethyl derivatives are generally 4–8 times less active than the sulfates, but their activity is difficult to measure precisely since on incubation they spontaneously decay to the parent compound, with a corresponding progressive increase in antibacterial activity.
Binding of polymyxins to the bacterial cell membrane can increase permeability to hydrophilic compounds, including sulfonamides and trimethoprim, producing significant synergy. Synergy with ciprofloxacin is also described. Calcium ions exert a strong pH-dependent competition for membrane binding sites, and the presence of calcium and magnesium ions in certain culture media adversely affects the bactericidal activity, notably against Ps. aeruginosa.

Acquired resistance

There is complete cross-resistance between the polymyxins, but stable acquired resistance in normally susceptible species is very rare. Adaptive resistance, probably due to changes in cell-wall permeability, is readily achieved by passage of a variety of enterobacteria in the presence of the agents in vitro.

General Description

In 1950, Koyama et al. isolated an antibiotic fromAerobacillus colistinus (B. polymyxa var. colistinus) thatwas given the name colistin (Coly-Mycin S). It was used inJapan and in some European countries for several years beforeit was made available for medicinal use in the UnitedStates. It is recommended especially for the treatment of refractory urinary tract infections caused by Gram-negativeorganisms such as Aerobacter, Bordetella, Escherichia,Klebsiella, Pseudomonas, Salmonella, and Shigella spp.
Chemically, colistin is a polypeptide, reported by Suzukiet al. whose major component is colistin A. They proposedthe structure for colistin A differs from polymyxin B only by the substitution of D-leucine for D-phenylalanine as one of the amino acid fragments inthe cyclic portion of the structure. Wilkinson and Lowehave corroborated the structure and have shown that colistinA is identical with polymyxin E1.
Two forms of colistin have been prepared, the sulfate andmethanesulfonate, and both forms are available for use in theUnited States. The sulfate is used to make an oral pediatricsuspension; the methanesulfonate is used to make an intramuscularinjection. In the dry state, the salts are stable, andtheir aqueous solutions are relatively stable at acid pH from 2to 6. Above pH 6, solutions of the salts are much less stable.

Hazard

A poison by ingestion.

Pharmaceutical Applications

Polymyxin B and colistin (polymyxin E); mixtures of sulfates of polypeptides produced by strains of B. polymyxa and B. polymyxa var. colistinus. Colistimethate sodium (colistin sulfomethate sodium). Molecular weights: polymyxin B 1 1203; polymyxin B 2 1189; colistimethate sodium 1748.
A group of basic polypeptide antibiotics with a side chain terminated by characteristic fatty acids. Five polymyxins (A–E) were originally characterized and others have since been added. Polymyxin B and colistin (polymyxin E) sulfates have been commercially developed.
By treatment with formalin and sodium bisulfite, five of the six diaminobutyric acid groups of the polymyxins can be modified by sulfomethyl groups to form undefined mixtures of the mono-, di-, tri-, tetra- and penta-substituted derivatives. Sulfomethyl polymyxins differ considerably in their properties from the parent antibiotics: they are less active antibacterially, less painful on injection, more rapidly excreted by the kidney and less toxic. Only colistimethate sodium is now commercially available for systemic use, but polymyxin B and colistin sulfates are found as ingredients of several topical formulations.

Biochem/physiol Actions

Mode of Action: Binds to lipids on the cell cytoplasmic membrane of Gram-negative bacteria and disrupts the cell wall integrity. Antimicrobial spectrum: Gram-negative bacteria. It is proposed that renal reabsorption of colistin may involve organic cation transporters and peptide transporters and that the process is sensitive to pH .

Pharmacokinetics

Oral absorption: Negligible
Cmax (colistimethate sodium) 2 mega-units: 6–7 mg/L after 2–3 h
(c. 16 mg colistin base) i.m.
Plasma half-life (colistimethate sodium): c.4–6 h
Plasma protein binding: Very low
Absorption
Polymyxins are not absorbed from the alimentary tract or mucosal surfaces, but can be absorbed from denuded areas or large burns.
Distribution
After parenteral administration of the sulfates, blood levels are usually low (1–4 mg/L 2 h after a 500 000 unit intramuscular dose). Substantially higher plasma levels are obtained from intramuscular injections of sulfomethyl polymyxins. There is some accumulation in patients receiving 120 mg every 8 h. In patients treated intravenously with a priming dose of 1.5–2.5 mg/kg followed by continuous infusion of 4.8–6.0 mg/h for 20–30 h, steady state levels were around 5–10 mg/L. The volume of distribution is unknown, but polymyxins diffuse poorly into tissue fluids and penetration to cerebrospinal fluid is poor. As a result of binding to mammalian cell membranes (sulfomethates less so), they persist in the tissues, where they accumulate on repeated dosage, although they disappear from the serum. Polymyxin crosses the placenta, but the levels achieved are low. A small amount appears in the breast milk.
Metabolism and excretion
The sulfates are excreted almost entirely by the kidney, but after a considerable lag, with very little of the dose appearing in the first 12 h. The sulfomethyl derivatives are much more rapidly excreted, accounting for their shorter half-lives. Around 80% of a parenteral dose of colistimethate sodium is eventually found in the urine, with concentrations reaching around 100–300 mg/L at 2 h. The fate of the remainder is unknown, but no metabolic products have been described and none is excreted in the bile. Polymyxins accumulate in renal failure and are not removed by peritoneal dialysis.

Clinical Use

Colistimethate sodium
Infections due to Ps. aeruginosa and other Gram-negative rods resistant to less toxic agents
Cystic fibrosis (inhalation therapy for pseudomonas infection)
Polymyxin B and colistin sulfate
Component of preparations for local application
Superficial infections with Ps. aeruginosa and to prevent the colonization of burns
Selective decontamination of the gut and as a paste for control of upper respiratory tract colonization in patients on prolonged mechanical ventilation (in combination with other agents)

Side effects

Pain and tissue injury can occur at the site of injection of the sulfates, but this is less of a problem with the sulfomethyl derivatives. Neurological symptoms such as paresthesia with typical numbness and tingling around the mouth, dizziness and weakness are relatively common, and neuromuscular blockade, sometimes severe enough to impede respiration, occurs. Evidence of nephrotoxicity is observed in about 20% of patients, leading to acute tubular necrosis in about 2%. Damage is more likely in patients with pre-existing renal disease. The appearance of any evidence of deterioration of renal function or of neuromuscular blockade calls for immediate cessation of treatment. All the toxic manifestations appear to be reversible, but complete recovery may be slow.
Although less toxic than the sulfate, untoward effects have been observed in up to one-quarter of those treated with colistimethate sodium. Nephrotoxicity is common, with an increase in urea and creatinine over the first few days of treatment. Acute tubular necrosis is heralded by the appearance of proteinuria, hematuria and casts, sometimes without prior evidence of functional impairment. Renal damage usually continues to progress for up to 2 weeks after withdrawal of therapy. Renal damage is likely to increase with the dose and with the simultaneous administration of other potentially nephrotoxic agents. Manifestations of central and peripheral neurotoxicity occur particularly in patients with impaired renal function. Neuromuscular blockade is seen principally in patients also receiving anesthetics or other agents that impair neuromuscular transmission. Complete flaccid paralysis with respiratory arrest and subsequent complete recovery has been seen in a patient with myasthenia gravis. Allergy is occasionally seen, and nebulized colistin has caused bronchial hyperreactivity with tightness in the chest in adults with cystic fibrosis. Application of colistin or polymyxin B ear drops can lead to ototoxicity.

Safety Profile

A poison by ingestion, intraperitoneal, subcutaneous, and intravenous routes. When heated to decomposition it emits toxic vapors of NOx and SOx.

Colistin sulfate Preparation Products And Raw materials

Raw materials

Preparation Products

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Colistin sulfate Suppliers

XiaoGan ShenYuan ChemPharm co,ltd
Tel
0712-0712-2580635 15527768850
Email
1791901229@qq.com
Country
China
ProdList
8850
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52
Wuhan DingCheng Biochemical Co.Ltd
Tel
027-81302558 13545255233
Email
2851686513@qq.com
Country
China
ProdList
843
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58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
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future industrial shanghai co., ltd
Tel
400-0066400 13621662912
Fax
021-55660885
Email
sales@jonln.com
Country
China
ProdList
1998
Advantage
65
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6013
Advantage
61
TCI (Shanghai) Development Co., Ltd.
Tel
021-67121386
Fax
021-67121385
Email
Sales-CN@TCIchemicals.com
Country
China
ProdList
24539
Advantage
81
ShangHai DEMO Chemical Co.,Ltd
Tel
400-021-7337 2355568890
Fax
0086-21-50182339
Email
sales@demochem.com
Country
China
ProdList
2572
Advantage
57
Energy Chemical
Tel
021-021-58432009 400-005-6266
Fax
021-58436166
Email
sales8178@energy-chemical.com
Country
China
ProdList
44751
Advantage
61
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10194
Advantage
62
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View Lastest Price from Colistin sulfate manufacturers

Shaanxi TNJONE Pharmaceutical Co., Ltd
Product
Colistin Sulphate 1264-72-8
Price
US $0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000kg
Release date
2024-03-25
Sigma Audley
Product
Colistin sulfate 1264-72-8
Price
US $35.00-25.00/kg
Min. Order
1kg
Purity
99.8%
Supply Ability
200tons/year
Release date
2024-03-12
shandong perfect biotechnology co.ltd
Product
Colistin sulfate 1264-72-8
Price
US $0.00/g
Min. Order
1g
Purity
98% HPLC
Supply Ability
1000kg
Release date
2023-08-04

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