| CAS NO: | 56377-79-8 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 1222.4 |
| Cas No. | 56377-79-8 |
| Formula | C51H43N13O12S6 |
| Synonyms | Multhiomycin,NSC 307240,RP 9671 |
| Solubility | Soluble in DMSO |
| Chemical Name | 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 SMILES | OC1=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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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