Linopristin

Names

[ CAS No. ]:
325965-23-9

[ Name ]:
Linopristin

[Synonym ]:
UNII-312V80FR4J
Linopristin [INN]
N-((6R,9S,10R,13S,15aS,22S,24aS)-22-((4-(dimethylamino)phenyl)methyl)-6-ethyl-10,23-dimethyl-18-((morpholin-4-yl)methyl)-5,8,12,15,21,24-hexaoxo-13-phenyl-1,2,3,5,6,7,8,9,10,11,12,13,14,15,15a,16,19,21,22,23,24,24a-docosahydropyrido(2,1-f)pyrrolo(2,1-l)(1,4,7,10,13,16)oxapentaazacyclononadecin-9-yl)-3-hydroxypyridine-2-carboxamide

Biological Activity

[Description]:

Linopristin is a kind of type B streptogramin antibiotics. Linopristin, together with type A, Flopristin, to form the streptogramin combination NXL 103. Linopristin exhibit synergistic antimicrobial activity against certain pathogenic bacteria with Flopristin. The preference ratio of Linopristin/Flopristin is 30:70 (w/w) or 70 μM Linopristin +120 μM Flopristin[1].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Linopristin (0-64 μg/mL) 对革兰氏阴性病原菌的抑菌作用不大，原因是其外细胞膜渗透性差[1]。 Linopristin 抑制粪肠球菌、金黄色葡萄球菌和肺炎葡萄球菌的生长，IC50 分别为 8 μg/mL、32 μg/mL 和 4 μg/mL[1]。

[References]

[1]. Noeske J, et al. Synergy of streptogramin antibiotics occurs independently of their effects on translation. Antimicrob Agents Chemother. 2014 Sep;58(9):5269-79.  

Chemical & Physical Properties

[ Molecular Formula ]:
C50H63N9O10

[ Molecular Weight ]:
950.09000

[ Exact Mass ]:
949.47000

[ PSA ]:
233.83000

[ LogP ]:
2.44760

Related Compounds