Product Data?SheetGamithromycinCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-108365145435-72-9C??H??N?O??777.04BacterialAnti-infectionPowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : 100 mg/mL (128.69 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM1.2869 mL0.2574 mL0.1287 mL6.4347 mL1.2869 mL0.6435 mL12.8694 mL2.5739 mL1.2869 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；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (3.22 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (3.22 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-CD in saline)Solubility: 2.5 mg/mL (3.22 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemExpress.cn
此?案可获得 2.5 mg/mL (3.22 mM) 的均匀悬浊液，悬浊液可?于?服和腹腔注射。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。3. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (3.22 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (3.22 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性Gamithromycin 是?种可以抑制 MmmSC 菌株 B237 和 Tan8 ?长的抗菌剂，MIC 值分别为 0.00012 和 0.00006 μg/mL。IC?? & Target体外研究MIC: 0.00012 μg/mL (MmmSC strain B237), 0.00006μg/mL (MmmSC strain Tan8)[1]The MIC values in serum are significantly lower than those in artificial medium; at an initial inoculum size of 106 cfu/mL, these are 64-, 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 serum or artificial medium[1].体内研究The proportion of foals that recover without the need for a change in treatment is significantly (P<0.048) higher for foals treated with Gamithromycin (GAM) (38 of 40; 95%) or AZM-RIF (39 of 40; 98%) compare to control foals (32 of 41; 78%). The clinical scores, number of abscesses and the abscess scores after 1 and 2 weeks of treatment are significantly lower for foals treated with Gamithromycin (GAM) or AZM-RIF compare to control foals. The WBC count of foals treated with Gamithromycin (GAM) is significantly higher than that of foals treated with AZM-RIF on week 3 of treatment[2].PROTOCOLCell Assay [1]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].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [2]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].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3
www.MedChemExpress.cn
REFERENCES
[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.
McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: tech@MedChemExpress.cn
Master of Small Molecules — 您?边的抑制剂?师
Page 3 of 3 www.MedChemExpress.cn
相关推荐：
loading