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colistimethate

Names

[ CAS No. ]:
12705-41-8

[ Name ]:
colistimethate

[Synonym ]:
{[(3S)-4-{[(3S,6S,9S,12S,15R,18S,21S)-3-[(1R)-1-Hydroxyethyl]-12,15-diisobutyl-2,5,8,11,14,17,20-heptaoxo-6,9,18-tris{2-[(sulfomethyl)amino]ethyl}-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]amino}-3-{[(2S,3R)-3-hydroxy-2-({(2S)-2-[(6-methylheptanoyl)amino]-4-[(sulfomethyl)amino]butanoyl}amino)butanoyl]amino}-4-oxobutyl]amino}methanesulfonic acid
2,6,9,14-Tetraazapentadecane-1,15-disulfonic acid, 8-[(1R)-1-hydroxyethyl]-5-[[[(3S,6S,9S,12S,15R,18S,21S)-3-[(1R)-1-hydroxyethyl]-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-6,9,18-tris[2-[(sulfomethyl)amino]ethyl]-1,4,7,10,13,16,19-heptaazacyclotricos-21-yl]amino]carbonyl]-11-[(6-methyl-1-oxoheptyl)amino]-7,10-dioxo-, (5S,8S,11S)-

Biological Activity

[Description]:

Colistimethate is a polymyxin with cytotoxicity to renal tubular cells. Colistimethate has poorly inactive in vivo. Colistimethate shows seldomly detectable activity against 6 strains of P. aeruginosa[1][2].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> Others >> Others

[In Vitro]

Colistimethate 对肾小管细胞有细胞毒性[1]。

[In Vivo]

Colistimethate 容易在体内引起肾毒性[1]。 Colistimethate (306 mg/kg; 皮下注射; 单次剂量) 在小鼠体内对 P. aeruginosa 菌株 (i.p.) 相对无效[2]。

[References]

[1]. Zavascki AP, et al. Nephrotoxicity of Polymyxins: Is There Any Difference between Colistimethate and Polymyxin B? Antimicrob Agents Chemother. 2017 Feb 23;61(3):e02319-16.  

[2]. Davis SD. Activity of gentamicin, tobramycin, polymyxin B, and colistimethate in mouse protection tests with Pseudomonas aeruginosa. Antimicrob Agents Chemother. 1975 Jul;8(1):50-3.  

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C57H108N16O28S5

[ Molecular Weight ]:
1625.883

[ Exact Mass ]:
1624.612305

[ LogP ]:
-12.35

[ Index of Refraction ]:
1.609

Related Compounds