Gamithromycin-ML-1709460-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGamithromycinCat. No.: HY-108365CAS No.: 145435-72-9Synonyms: ML-1709460分式: CHNO分量: 777.04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 : 160 mg/mL (205.91

2、mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.2869 mL 6.4347 mL 12.8694 mL5 mM 0.2574 mL 1.2869 mL 2.5739 mL10 mM 0.1287 mL 0.6435 mL 1.2869 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 Gamithromycin种可以抑制 MmmSC 株 B237 和 Tan8 长的抗菌剂，MIC 值分

3、别为 0.00012 和0.00006 g/mL。IC50 & Target MIC: 0.00012 g/mL (MmmSC strain B237), 0.00006g/mL (MmmSC strain Tan8) 1体外研究The MIC values in serum are significantly lower than those in artificial medium; at an initial inoculum size of1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE106 cfu/mL, these are 64-

4、, 8- and 64-fold lower for gamithromycin, tylosin and tilmicosin, respectively,against MmmSC strain B237 in serum compare to artificial medium. A similar pattern emerges for Tan8.Heat-inactivation of serum results in an MIC for gamithromycin that is higher than in either non-treated serumor artifici

5、al medium 1.体内研究 The proportion of foals that recover without the need for a change in treatment is significantly (P 2.PROTOCOLCell Assay 1 Minimum inhibitory concentrations (MICs) for gamithromycin, tylosin and tilmicosin against MmmSC strainsB237 and Tan8 are determined using a macrodilution techn

6、ique. Equal volumes of MmmSC culture inlogarithmic phase are added to each antimicrobial dilution to give an inoculum size of 107 cfu/mL, i.e. theintending initial titre for subsequent time-kill assays, in a volume of 4 mL. Cultures are incubated for 24 h at37C. At 0 and 24 h time points, samples ar

7、e removed and serially diluted 10-fold down to 10-5. Aliquots (10L) of each dilution are transferred to solid medium; after incubation at 37C in a humidified atmosphere of5% carbon dioxide in air for at least 4 days, colonies are counted from the dilution that yields between 30 and300 colonies per p

8、late. Counts are converted into cfu/mL and MIC is defined as the lowest concentration ofantimicrobial that prevents an increase in cfu/mL over 24 h 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Foals with ultrasonographic evidence of pulmonar

9、y abscesses are randomly assigned in 3 treatment groups:Administration 2 (1)gamithromycin at a dose of 6.0 mg/kg body weight is administered in thesemimembranosus/semitendinosus muscles once a week (GAM; n=40); (2) azithromycin at a dose of 10mg/kg PO once daily in combination with rifampin at a dos

10、e of 10 mg/kg PO once daily (AZM-RIF; n=40); and(3) no antimicrobial treatment (controls; n=41). All the foals in each treatment group also receiveacetylcysteine at a dose of 10 mg/kg PO a day to provide the same daily manipulation of the foals in eachgroup 2.MCE has not independently confirmed the

11、accuracy of these methods. They are for reference only.REFERENCES1. Mitchell JD, et al. In vitro pharmacodynamics of gamithromycin against Mycoplasma mycoides subspecies mycoides Small Colony. VetJ. 2013 Sep;197(3):806-11.2. F. Hildebrand, et al. Efficacy of Gamithromycin for the Treatment of Foals with Mild to Moderate Bronchopneumonia. J Vet Intern Med.2015 Jan-Feb; 29(1): 333338.McePdfHeightCaution: Product has