Nosiheptide-Multhiomycin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENosiheptideCat. No.: HY-107486CAS No.: 56377-79-8Synonyms: Multhiomycin; RP 9671分式: CHNOS分量: 1222.36作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/m

2、L (102.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.8181 mL 4.0904 mL 8.1809 mL5 mM 0.1636 mL 0.8181 mL 1.6362 mL10 mM 0.0818 mL 0.4090 mL 0.8181 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Nosiheptide (Multhiomycin)种由 Streptomyces actuosus 产的硫

3、肽抗素，可抑制细蛋质的合成，并在独特的环核上具有独特的吲哚侧环系统和区域特异性羟，已被泛作动物长的饲料添加剂。体外研究Nosiheptide exhibits extremely potent activity against all contemporary Staphylococcus aureus strains testedincluding multiple drug-resistant clinical isolates, with MIC values 0.25 mg/L. Nosiheptide is also highlyactive against Enterococcus

4、 spp and the contemporary hypervirulent BI strain of Clostridium difficile but is1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEinactive against most Gram-negative strains tested. Time-kill analysis reveals Nosiheptide to be rapidlybactericidal against Staphylococcus aureus in a concentration- and

5、 time-dependent manner, with a nearly 2-log kill noted at 6 hours at 10X MIC. Furthermore, Nosiheptide is found to be non-cytotoxic againstmammalian cells at 100X MIC, and its anti-Staphylococcus aureus activity is not inhibited by 20% humanserum. Notably, Nosiheptide exhibits a significantly prolon

6、ged post-antibiotic effect against both healthcare-and community-associated Staphylococcus aureus compared to vancomycin 1.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 t

7、he Nosiheptide-treated mice remains aliveon day 3, while 6/10 of the controls died on day 1 1.Animal Model: Eight week old female CD1 mice injected with HA-Staphylococcus aureus strain Sanger252 1Dosage: 20 mg/kgAdministration: Intraperitoneal injection; injected at 1 and 8 h post-infectionResult: P

8、rovided significant protection against mortality.REFERENCES1. Haste NM, et al. Activity of the thiopeptide antibiotic nosiheptide against contemporary strains of methicillin-resistant Staphylococcusaureus. J Antibiot (Tokyo). 2012 Dec;65(12):593-8.2. Yu Y, et al. Nosiheptide biosynthesis featuring a unique indole side ring formation on the characteristic thiopeptide framework. ACSChem Biol. 2009 Oct 16;4(10):855-64.McePdfHeightCaution: Product has not been fully validated for medical applic