|(2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-11-(((2S,3R,4S,6R)-4-(二甲基氨基)-3-羟基-6-甲基四氢-2H-吡喃-2-基)氧基)-2-乙基-3,4,10-三羟基-13-(((2R,4R,5S,6S)-2R,4R,5S,6S)-5-羟基-4-甲氧基-4,6-二甲基四氢-2H-吡喃-2-基)氧基)-3,5,8,10,12,14-六甲基-7-丙基-1-氧杂-7-氮杂环十五烷-15-酮|CsnPharm

CAS No.: 145435-72-9

Gamithromycin/加米霉素 Catalog No. CSN23819

Synonyms: ML-1709460;GAM;加米霉素

Gamithromycin is an antibiotic that is active against macrolide-resistant R. equi and S. zooepidemicus with MIC90s = 1 and 0.125 μg/ml, respectively.

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技术信息

生物活性

描述Gamithromycin is an antimicrobial agent which can inhibit the growth of MmmSC strains B237 and Tan8 with MICs of 0.00012 and 0.00006 μg/mL, respectively. All three antimicrobials were mycoplasmastatic with maximum effects of -0.44, -0.32 and -0.49log10(cfu/mL) units for gamithromycin, tylosin and tilmicosin, respectively, against B237 in artificial medium^[1]. Gamithromycin is active in vitro against the bacterial agents most commonly associated with bronchopneumonia in older foals^[2]. The minimum inhibitory concentration (MIC) of gamithromycin against P. multocida in mice serum was 0.15 μg/ml. Analysis of PK/PD indices using the inhibitory effect E max model indicated a strong correlation (R 2 = 0.9624) between the f AUC0-24/MIC ratio and various antibacterial effects^[3]. The MIC of gamithromycin for macrolide-resistant R. equi isolates (MIC(90)=128 μg/mL) was significantly higher than that for macrolide-susceptible isolates (1.0 μg/mL). The activity of gamithromycin against intracellular R. equi was similar to that of azithromycin and erythromycin. Intramuscular administration of gamithromycin at a dosage of 6 mg/kg would maintain PELF concentrations above the MIC(90) for S. zooepidemicus and phagocytic cell concentrations above the MIC(90) for R. equi for approximately 7 days^[4].
参考文献

[1] Mitchell JD, Goh S, McKellar QA, McKeever DJ. In vitro pharmacodynamics of gamithromycin against Mycoplasma mycoides subspecies mycoides Small Colony. Vet J. 2013;197(3):806‐811
[2] Hildebrand F, Venner M, Giguère S. Efficacy of gamithromycin for the treatment of foals with mild to moderate bronchopneumonia. J Vet Intern Med. 2015;29(1):333‐338
[3] Yang Q, Liu X, Zhang C, et al. Pharmacokinetics and Pharmacodynamics of Gamithromycin Treatment of Pasteurella multocida in a Murine Lung Infection Model. Front Pharmacol. 2019;10:1090. Published 2019 Sep 24
[4] Berghaus LJ, Giguère S, Sturgill TL, Bade D, Malinski TJ, Huang R. Plasma pharmacokinetics, pulmonary distribution, and in vitro activity of gamithromycin in foals. J Vet Pharmacol Ther. 2012;35(1):59‐66

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2869 mL
- 6.4347 mL
- 12.8694 mL
- 5 mM
- 0.2574 mL
- 1.2869 mL
- 2.5739 mL
- 10 mM
- 0.1287 mL
- 0.6435 mL
- 1.2869 mL

技术信息

CAS号

145435-72-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C40H76N2O12

运输

蓝冰

分子量

777.04

别名

ML-1709460;GAM;加米霉素

溶解度

DMSO	98.0 mg/mL (126.1 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (128.7 mM)

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