中文名 | 诺西肽 |
英文名 | Nosiheptide |
别名 | 那西肽 诺西肽 诺肽菌素 那西肽NOSIHEPTIDE |
英文别名 | 101159 CS-2680 priMofax Nosiheptide Multhiomycin Nosiheptide VETRANAL Nosiheptide (Multhiomycin) |
CAS | 56377-79-8 |
EINECS | 260-138-4 |
化学式 | C51H43N13O12S6 |
分子量 | 1222.34 |
InChI | InChI=1/C51H43N13O12S6/c1-5-23-46-60-28(14-79-46)41(70)56-25-10-33(67)50(74)76-11-21-7-6-8-24-34(21)18(2)35(54-24)51(75)82-17-31(57-42(71)29-15-80-47(25)61-29)48-58-26(12-78-48)37-22(45-59-30(13-77-45)43(72)64-36(20(4)65)44(73)55-23)9-32(66)38(63-37)49-62-27(16-81-49)40(69)53-19(3)39(52)68/h5-9,12-16,20,25,31,33,36,54,65-67H,3,10-11,17H2,1-2,4H3,(H2,52,68)(H,53,69)(H,55,73)(H,56,70)(H,57,71)(H,64,72)/b23-5- |
密度 | 1.534±0.06 g/cm3(Predicted) |
熔点 | 310-320° (dec) |
比旋光度 | D20 +38° (c = 1 in pyridine) |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
折射率 | 1.698 |
酸度系数 | 1.42±0.60(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Light Yellow to Light Brown |
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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