NosiheptideCAS号: 56377-79-8分子式: C51H43N13O12S6分子量: 1222.36描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
Nosiheptide is a bicyclic thiopeptide antibiotic produced by several species of actinomycetes, notably Streptomyces.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
那西肽; Multhiomycin;RP 9671
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| 外观 |
white to beige powder
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| 可溶性/溶解性 |
DMSO : 125 mg/mL (102.26 mM; Need ultrasonic)
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| 生物活性 | |
| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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.
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分子结构图
