那西肽
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 |
那西肽 用途与合成方法
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. |
