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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETedizolid phosphateCat. No.: HY-14855BCAS No.: 856867-55-5Synonyms: TR-701FA分式: CHFNOP分量: 450.32作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 36 mg/mL (79
2、.94 mM)H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2206 mL 11.1032 mL 22.2064 mL5 mM 0.4441 mL 2.2206 mL 4.4413 mL10 mM 0.2221 mL 1.1103 mL 2.2206 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIV
3、ITY物活性 Torezolid磷酸鹽MAO-A和MAO-B抑制劑,具有抗蘭陽(yáng)性菌的活性。體外研究 Tedizolid (0.25 g/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid againstPRSP 1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 For mice infected with PSSP type III, the 100% survival rate is achieved wit
4、h tedizolid phosphate at aminimum total daily dose of 10 mg/kg. Lungs of infected mice treated with tedizolid phosphate show lesssevere inflammation and edema, as indicated by the mean scores for inflammation and edema 1.PROTOCOLAnimal To induce a systemic S. pneumoniae infection, male ICR mice (wei
5、ght, 18 to 20 g) are inoculatedAdministration 1 intraperitoneally with 1 of 4 PRSP isolates (DR9, DR10, DR11, or DR14) suspended in 10% mucin. Thesuspension contained sufficient bacteria to kill 100% of untreated control mice. At 1 h postinfection, micereceives a single dose of either tedizolid phos
6、phate or linezolid, and survival is assessed daily for 7 dayspostinfection. Treatments are delivered both orally and intravenously at each of four doses (40 mg/kg of bodyweight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg), with 8 mice per group defined by dose, delivery method,and infecting strain. The
7、 50% effective dose (ED50), i.e., the dose allowing survival of 50% of the infectedmice, is calculated for each delivery route using probit analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Front Microbiol. 2018 Sep 7;9:2095. J Pharm
8、Biomed Anal. 2019 May 30;169:170-180. J Pharm Biomed Anal. 2017 May 30;139:221-231. J Pharm Biomed Anal. 2016 Feb 20;120:402-12. Journal of Molecular Structure. 2016 Jul 5; 1115:136-143.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Choi S, et al. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitiveStreptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19.McePdfHeightCaution: Product has not been fully validated for medical appl
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