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Gamithromycin (ML-1709460)

An antibiotic

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  • 货号: ajce48466
  • CAS: 145435-72-9
  • 别名: 加米霉素; ML-1709460
  • 分子式: C40H76N2O12
  • 分子量: 777.04
  • 纯度: >98%
  • 溶解度: DMSO : 160 mg/mL (205.91 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Gamithromycin is an antibiotic that is active against macrolide-resistant R. equi and S. zooepidemicus (MIC90s = 1 and 0.125 μg/ml, respectively).1 It reduces the number of pneumonic lesions in a bovine M. haemolytica challenge model at a dose of 6 mg/kg.2 Formulations containing gamithromycin have been used to treat bovine respiratory diseases.3


1.Berghaus, L.J., Giguère, S., Sturgill, T.L., et al.Plasma pharmacokinetics, pulmonary distribution, and in vitro activity of gamithromycin in foalsJ. Vet. Pharmacol. Ther.35(1)59-66(2012) 2.Forbes, A.B., Ramage, C., Sales, J., et al.Determination of the duration of antibacterial efficacy following administration of gamithromycin using a bovine Mannheimia haemolytica challenge modelAntimicrob. Agents Chemother.55(2)831-835(2011) 3.Capik, S.F., White, B.J., Lubbers, B.V., et al.Comparison of the diagnostic performance of bacterial culture of nasopharyngeal swab and bronchoalveolar lavage fluid samples obtained from calves with bovine respiratory diseaseAm. J. Vet. Res.78(3)350-358(2017)

Protocol

Cell experiment:

Minimum inhibitory concentrations (MICs) for gamithromycin, tylosin and tilmicosin against MmmSC strains B237 and Tan8 are determined using a macrodilution technique. Equal volumes of MmmSC culture in logarithmic phase are added to each antimicrobial dilution to give an inoculum size of 107 cfu/mL, i.e. the intending initial titre for subsequent time-kill assays, in a volume of 4 mL. Cultures are incubated for 24 h at 37°C. At 0 and 24 h time points, samples are removed and serially diluted 10-fold down to 10-5. Aliquots (10 μL) of each dilution are transferred to solid medium; after incubation at 37°C in a humidified atmosphere of 5% carbon dioxide in air for at least 4 days, colonies are counted from the dilution that yields between 30 and 300 colonies per plate. Counts are converted into cfu/mL and MIC is defined as the lowest concentration of antimicrobial that prevents an increase in cfu/mL over 24 h[1].

Animal experiment:

Foals with ultrasonographic evidence of pulmonary abscesses are randomly assigned in 3 treatment groups: (1)gamithromycin at a dose of 6.0 mg/kg body weight is administered in the semimembranosus/semitendinosus muscles once a week (GAM; n=40); (2) azithromycin at a dose of 10 mg/kg PO once daily in combination with rifampin at a dose 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 receive acetylcysteine at a dose of 10 mg/kg PO a day to provide the same daily manipulation of the foals in each group[2].

参考文献:

[1]. Mitchell JD, et al. In vitro pharmacodynamics of gamithromycin against Mycoplasma mycoides subspecies mycoides Small Colony. Vet J. 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): 333–338.

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