那西肽

生物活性体外研究体内研究那西肽试剂级价格

那西肽

CAS号:56377-79-8
英文名:Nosiheptide
中文名:那西肽
CBNumber:CB2875431
分子式:C51H43N13O12S6
分子量:1222.34
MOL File:56377-79-8.mol

那西肽化学性质

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 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :1.42±0.60(Predicted)
颜色 :Light Yellow to Light Brown

那西肽性质、用途与生产工艺

生物活性 Nosiheptide (Multhiomycin) 是一种由 Streptomyces actuosus 产生的硫肽抗生素，可抑制细菌蛋白质的合成，并在独特的大环核上具有独特的吲哚侧环系统和区域特异性羟基，已被广泛用作动物生长的饲料添加剂。
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.

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.

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.