145435-72-9

• 常用中文名：加米霉素
• 常用英文名：Gamithromycin
• CAS号：145435-72-9
• 分子式：C₄₀H₇₆N₂O₁₂
• 分子量：777.038
• 相关类别： 原料药 抗生素类药物 多肽类药
• 发布时间：2018-09-08 11:37:07
• 更新时间：2026-07-09 14:54:27
• Gamithromycin 是一种可以抑制 MmmSC 菌株 B237 和 Tan8 生长的抗菌剂,MIC 值分别为 0.00012 和 0.00006 μg/mL。

名称

• 中文名: 加米霉素
• 英文名: gamithromycin
• 中文别名: 加米霉素及中间体; 化合物：Gamithromycin (ML-1709460); 加密霉素; 加米霉素溶液, 100PPM; 加米霉素检测标准品; 加米霉素,10 MM DMSO 溶液; 加米霉素标准品; 加米红霉素; Gamithromycin 甲米霉素; 化合物:Gamithromycin (ML-1709460); (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; gamithromycin ,加米霉素; 加米霉素原粉; Veteriny antibiotic13加米霉素
• 英文别名: (2R,3S,4R,5S,8R,10R,11R,12S,13R,14S)-11-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-ethyl-3,4,10-trihydroxy-13-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3,5,8,10,12,14-hexamethyl; Zactran; Gamithromycin 100 μg/mL in Methanol; 1-Oxa-7-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R); Camithromycin; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-Cmethyl-3-O-methyl-a-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-b-D-xylo-hexopyranosyl]oxy]-1-oxa-7-azacyclopentadecan-15-one; Tianfu Chem Gamithromycin; Gamma mycin; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-2-Ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-15-oxo-7-propyl-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-7-azacyclopentadecan-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranoside; Gamithromycin, 10 mM in DMSO; GAMITHROMYCIN; Disodium 4,5-dihydro-4,5-dioxo-1H-pyrrolo(2,3-f)quinoline-2,7,9-tricboxylate; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-Cmet; gamimycin; Gamithromycin Solution, 100ppm; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-11-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-ethyl-3,4,10-trihydroxy-13-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3,5,8,10,12,14-hexamethyl; 1-Oxa-7-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo; Gamithromycin //BP; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-11-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-ethyl-3,4,10-trihydroxy-13-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3,5,8,10,12,14-hexamethyl-7-propyl-1-oxa-7-azacyclopentadecan-15-one; Gamithromycin ,25; ML 1709460,GAMITHROMYCIN; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-7-azacylopentadecan-15-one; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-CMethyl-3-O-Methyl-a-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexaMethyl-7-propyl-11-[[3,4,6-trideoxy-3-(diMethylaMino)-b-D-xylo-hexopyranosyl]oxy]-1-oxa-7-azacyclopentadeca; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-Cmethyl-3-O-methyl-a-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-[[3,4,6-trideoxy-3-(dimethylamino; (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-Dideoxy-3-C-Methyl-3-O-Methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexaMethyl-7-propyl-11-[[3,4,6-trideoxy-3-(diMethylaMino)-β-D-xylo-hexopyranosyl]oxy]-1-oxa-7-azacyclopentadecan-15-one; Gamomycin; Gamithormycin

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 833.0±65.0 °C at 760 mmHg
• 分子式: C₄₀H₇₆N₂O₁₂
• 分子量: 777.038
• 闪点: 457.6±34.3 °C
• 精确质量: 776.539856
• PSA: 180.08000
• LogP: 3.89
• 蒸汽压: 0.0±0.6 mmHg at 25°C
• 折射率: 1.535
• 储存条件: 室温，干燥，密封

生物活性

• 描述: Gamithromycin 是一种可以抑制 MmmSC 菌株 B237 和 Tan8 生长的抗菌剂,MIC 值分别为 0.00012 和 0.00006 μg/mL。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染
• 靶点:

  MIC: 0.00012 μg/mL (MmmSC strain B237), 0.00006μg/mL (MmmSC strain Tan8)[1]

• 体外研究: 血清MIC值明显低于人工培养基;在初始接种量为106cfu/mL时,与人工培养基相比,血清中MmmSC菌株B237的gamithromycin,泰乐菌素和替米考星分别低64和8倍。 Tan8也出现了类似的模式。血清的热灭活导致gamithromycin的MIC高于未处理的血清或人工培养基[1]。
• 体内研究: 对于用Gamithromycin(GAM)治疗的驹(38个中的38个; 95％)或AZM-RIF(39个中的40个; 98％),治疗后恢复而不需要改变治疗的驹的比例显着(P <0.048)与对照马驹相比(41个中的32个; 78％)。与对照马驹相比,用Gamithromycin(GAM)或AZM-RIF治疗的驹治疗1周和2周后的临床评分,脓肿次数和脓肿评分显着降低。在治疗的第3周,用Gamithromycin(GAM)治疗的驹的WBC计数显着高于用AZM-RIF治疗的驹的数量[2]。
• 细胞实验: 使用宏滴定技术测定gamithromycin，泰乐菌素和替米考星对MmmSC菌株B237和Tan8的最小抑制浓度（MIC）。将对数期的等体积MmmSC培养物加入到每种抗微生物稀释液中，得到107cfu / mL的接种物大小，即随后的时间杀灭测定的初始滴度，体积为4mL。将培养物在37℃下孵育24小时。在0和24小时时间点，取出样品并连续稀释10倍至10-5。将每种稀释液的等分试样（10μL）转移至固体培养基中;在37℃，5％二氧化碳的空气湿润气氛中培养至少4天后，从稀释液中计数菌落，每个平板产生30-300个菌落。计数转换为cfu / mL，MIC定义为抗菌剂的最低浓度，可防止24小时内cfu / mL的增加[1]。
• 动物实验: 在3个治疗组中随机分配具有肺脓肿的超声波证据的驹：（1）每周一次在半膜肌/半腱肌中施用剂量为6.0mg / kg体重的gamithromycin（GAM; n = 40）; （2）阿奇霉素，剂量为10 mg / kg PO，每日一次，与利福平合用，剂量为10 mg / kg PO，每日一次（AZM-RIF; n = 40）; （3）无抗菌处理（对照; n = 41）。每个治疗组中的所有驹也每天以10mg / kg PO的剂量接受乙酰半胱氨酸，以提供每组中马驹的相同日常操作[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.

安全

• 符号: GHS07, GHS08
• 信号词: Warning
• 危害声明: H315-H319-H361d
• 警示性声明: P281-P305 + P351 + P338
• 危害码 (欧洲): Xi
• 危险品运输编码: NONH for all modes of transport