那西肽
| 中文名称 | 那西肽 |
|---|---|
| 中文同义词 | 那西肽1%预混粉;那西肽90%;那西肽;诺西肽;诺肽菌素;那西肽NOSIHEPTIDE;N-(3-氨基-3-氧代丙-1-烯-2-基)-2-((11S,14Z,21S,23S,29S)-14-亚乙基-3,23-二羟基-11-((1R)-(1-羟乙基))-31-甲基-9,12,19,24,33,43-六氧代-9,10,11,12,13,14,19,20,21,22,23,24,26,33,35,36-十六氢-21,36-([2,4]-ENDO-THIAZOLOMETHANIMINO)-5,8:15,18:37,40-三(AZENO)-30,32-EPIMINO苯并[H1]吡啶并[3,2-V][1]氧杂[10,20,26,30]四硫杂[6,13,16]三氮杂环三十六烷-2-基)噻唑-4;那西肽/诺肽菌素 |
| 英文名称 | Nosiheptide |
| 英文同义词 | Nosiheptide;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]-endo-thiazolomethanimino)-5H,15H,37H-pyrido[3,2-w][2,11,21,27,31,7,14,17]benzoxatetrathiatriazacyclohexatriacontin-2-yl]-4-thiazolecarboxamide;Nosiheptide VETRANAL;priMofax;Multhiomycin;Nosiheptide (Multhiomycin);101159;CS-2680 |
| CAS号 | 56377-79-8 |
| 分子式 | C51H43N13O12S6 |
| 分子量 | 1222.34 |
| EINECS号 | 260-138-4 |
| 相关类别 | 微生物代谢物;饲料添加剂 |
| Mol文件 | 56377-79-8.mol |
| 结构式 |  |
那西肽 性质
| 熔点 | 310-320° (dec) |
|---|---|
| 比旋光度 | D20 +38° (c = 1 in pyridine) |
| 密度 | 1.534±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 1.42±0.60(Predicted) |
| 颜色 | 浅黄色至浅棕色 |
Nosiheptide exhibits extremely potent activity against all contemporary Staphylococcus aureus strains tested including multiple drug-resistant clinical isolates, with MIC values ≤ 0.25 mg/L. Nosiheptide is also highly active against Enterococcus spp and the contemporary hypervirulent BI strain of Clostridium difficile but is inactive against most Gram-negative strains tested. Time-kill analysis reveals Nosiheptide to be rapidly bactericidal against Staphylococcus aureus in a concentration- and time-dependent manner, with a nearly 2-log kill noted at 6 hours at 10X MIC. Furthermore, Nosiheptide is found to be non-cytotoxic against mammalian cells at >> 100X MIC, and its anti- Staphylococcus aureus activity is not inhibited by 20% human serum. Notably, Nosiheptide exhibits a significantly prolonged post-antibiotic effect against both healthcare- and community-associated Staphylococcus aureus compared to vancomycin.
Nosiheptide (20 mg/kg; intraperitoneal injection; injected at 1 and 8 h post-infection; female CD1 mice) provids significant protection against mortality. Ten out of 10 of the Nosiheptide-treated mice remains alive on day 3, while 6/10 of the controls died on day 1.
| Animal Model: | Eight week old female CD1 mice injected with HA- Staphylococcus aureus strain Sanger 252 |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection; injected at 1 and 8 h post-infection |
| Result: | Provided significant protection against mortality. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-107486 | Nosiheptide | 1 mg | 666元 | |
| 2024/01/25 | HY-107486 | 那西肽 Nosiheptide | 56377-79-8 | 5mg | 2550元 |