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Nosiheptide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nosiheptide图片
CAS NO:56377-79-8
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Nosiheptide (Multhiomycin) 是一种由 Streptomyces actuosus 生产的硫肽类抗生素,可抑制细菌蛋白质合成,并在特征性的大环核心上带有独特的吲哚侧环系统和区域特异性羟基。
Cas No.56377-79-8
别名那西肽,Multhiomycin,NSC 307240,RP 9671
化学名N-[1-(aminocarbonyl)ethenyl]-2-[(11S,14Z,21S,23S,29S)-14-ethylidene-9,10,11,12,13,14,19,20,21,22,23,24,26,33,35,36-hexadecahydro-3,23-dihydroxy-11-[(1R)-1-hydroxyethyl]-31-methyl-9,12,19,24,33,43-hexaoxo-30,32-imino-8,5:18,15:40,37-trinitrilo-21,36-([2,4]
Canonical SMILESOC1=C(C2=NC(C(NC(C(N)=O)=C)=O)=CS2)N=C(C3=CSC([C@](NC(C4=CSC([C@](NC(C5=CSC(/C(NC([C@](NC(C6=CSC7=N6)=O)([H])[C@@H](O)C)=O)=C/C)=N5)=O)([H])C[C@H](O)C(OC8)=O)=N4)=O)([H])CSC(C9=C(C)C(C8=CC=C%10)=C%10N9)=O)=N3)C7=C1
分子式C51H43N13O12S6
分子量1222.4
溶解度DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MIC: ≤ 0.25 mg/L for methicillin-resistant S. aureus strains; ≤ 0.125 mg/L for Enterococcus spp; 0.008 mg/L for BI strain of C. difficile

Nosiheptide is a thiopeptide antibiotic.

Thiopeptides are a family of antibiotics counting with more than one hundred different entities. Although thiopeptides are mainly isolated from soil bacteria, new members have been isolated from marine samples. Thiopeptides have been reported to have a wide range of biological properties, such as antiplasmodial, anticancer, immunosuppressive, etc.

In vitro: The mode of action of nosiheptide on bacterial protein synthesis was found to be closely similar to that of thiostrepton. Both antibiotics could inhibit functions of elongation factors Tu and G and could also significantly reduce the synthesis of guanosine penta- and tetraphosphates to stringent factor. In addition, the actinomycetes that produced nosiheptide were able to defend themselves against their products in similar fashion, which involved specific pentosemethylation of 23s ribosomal RNA [1].

In vivo: The rHDL–nosiheptide complex was intravenously administered to male Wistar rats and the distribution of nosiheptide in the liver and plasma was monitored 30 min after injection. Results showed that the hepatic distribution of the rHDL–nosiheptide complex accounted for most of the administered nosiheptide, and was seven times as much as that in plasma. These findings indicated that the rHDL–nosiheptide complex could targete nosiheptide to the liver [2].

Clinical trial: Up to now, nosiheptide is still in the preclinical development stage.

References:
[1] E.  Cundliffe and J. Thompson. The mode of action of nosiheptide (multhiomycin) and the mechanism of resistance in the producing organism. J.Gen.Microbiol. 126(1), 185-192 (1981).
[2] Feng M, Cai Q, Shi X, Huang H, Zhou P, Guo X.  Recombinant high-density lipoprotein complex as a targeting system of nosiheptide to liver cells. J Drug Target. 2008 Jul;16(6):502-8.