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1264-72-8

1264-72-8 structure
1264-72-8 structure
  • Name: Colistin sulfate
  • Chemical Name: Colistin Sulfate
  • CAS Number: 1264-72-8
  • Molecular Formula: C52H100N16O17S
  • Molecular Weight: 1253.51
  • Catalog: API Antibiotics Other antibiotics
  • Create Date: 2018-02-08 08:00:00
  • Modify Date: 2024-01-02 13:21:28
  • Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Name Colistin Sulfate
Synonyms Polymyxin E
Polymyxin E
Colistin Sulphate
MFCD00146495
Colistin sulfate salt,Polymyxin E
Colistin sulfate salt
Colistin sulfate
EINECS 215-034-3
Colistin (sulfate)
Description Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Related Catalog
In Vitro Colistins are bactericidal to gram-negative bacteria by a detergent-like mechanism. This mechanism involves interaction with lipopolysaccharides and phospholipids of the outer membrane and electrostatic interference with the outer membrane by competitively displacing divalent cations (calcium and magnesium) from the negatively charged phosphate groups of membrane lipids[1]. Colistin (polymyxin E) owns favorable properties of rapid bacterial killing, a narrow spectrum of activity, and an associated slow development of resistance for the treatment of infections caused by multidrug-resistant gram-negative bacteria. There are two forms of colistin available commercially: colistin (sulfate) mainly for topical use and colistin methanesulfonate (sodium) for parenteral use[2].
In Vivo High concentrations of colistin in rat ELF are achieved as a result of slow and sustained CMS conversion following 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 rarely select for chromosomal resistance in the dominant E. coli population[4].
Animal Admin Rats: Colistin methanesulfonate (sodium) and colistin (sulfate) dosing solutions are freshly prepared in sterile 0.9% sodium chloride. For the i.v. studies, colistin methanesulfonate (CMS) or sulfate solutions are administered by a bolus injection via the jugular vein cannula. Intratracheal (i.t.) instillation is utilized as the technique for pulmonary administration. Animals are administered i.v. CMS at doses of 14 mg/kg of body weight, 28 mg/kg or 56 mg/kg. In an independent study, rats are administered i.v. colistin at doses of 0.21 mg/kg, 0.41 mg/kg, or 0.62 mg/kg[3].
References

[1]. Hancock RE et al. Peptide antibiotics. Antimicrob 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 from patients with cystic fibrosis. Antimicrob Agents Chemother. 2001 Mar;45(3):781-5.

[3]. W S Yapa S, et al. Population pharmacokinetics of colistin methanesulfonate in rats: achieving sustained lung concentrations of colistin for 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.
Density 1.3±0.1 g/cm3
Boiling Point 1537.3±65.0 °C at 760 mmHg
Melting Point 200-220°C
Molecular Formula C52H100N16O17S
Molecular Weight 1253.51
Flash Point 883.5±34.3 °C
PSA 573.64000
LogP -3.68
Vapour Pressure 0.0±0.6 mmHg at 25°C
Index of Refraction 1.575
Storage condition 2-8°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TR1500000
CHEMICAL NAME :
Polymyxin E sulfate
CAS REGISTRY NUMBER :
1264-72-8
LAST UPDATED :
199504
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C45-H85-N13-O10.H2-O4-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
72200 ug/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 13,7,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
793 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
21800 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
53500 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ABANAE Antibiotics Annual. (New York, NY) 1953-60. For publisher information, see AMACCQ. Volume(issue)/page/year: 7,41,1959/1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
58 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 16,105,1968 *** REVIEWS *** TOXICOLOGY REVIEW ANBCB3 Antibiotics and Chemotherapy (Basel). (S. Karger AG, Postfach CH-4009 Basel, Switzerland) V.17- 1971- Volume(issue)/page/year: 31,119,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M4682 No. of Facilities: 215 (estimated) No. of Industries: 2 No. of Occupations: 6 No. of Employees: 2247 (estimated) No. of Female Employees: 1438 (estimated)
Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements Missing Phrase - N15.00950417
Personal Protective Equipment Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes T:Toxic
Risk Phrases R25
Safety Phrases S45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS TR1500000
Packaging Group III
Hazard Class 6.1(b)
HS Code 2309901000
HS Code 2309901000

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