阿奇霉素二水物
中文名称:
阿奇霉素二水物
中文同义词:
9-脱氧-9a-氮杂-9a-红霉素A;阿奇霉素二水合物;阿齐霉素 二水合物;阿奇霉素(标准品);阿奇霉素二水物;阿奇霉素二水合物 标准品;A116-阿奇霉素二水物;(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-(((2S,3R,4S,6R)-4-(二甲基胺基)-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)-5-羟基-4-甲氧基-4,6-二甲基四氢-2H-吡喃-2-基)氧基]-3,5,6,8,10,12,14-七甲基-1-氧杂-6-氮杂环十五烷-15-酮二水合物
英文名称:
Azithromycin dihydrate
英文同义词:
AZITHROMYCIN 2-HYDRATE;1-Oxa-6-azacyclopentadecan-15-one, 13-(2,6-dideoxy-3-C-methyl-3-O-methyl-.alpha.-L-ribo-hexopyranosyl)oxy-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-3,4,6-trideoxy-3-(dimethylamino)-.beta.-D-xylo-hexopyranosyloxy-, dihydrate, (2R,3S,4R,5R,8;AZITHROMYCINDIHYDRATE(PATENTED-NOSUPPLY);1-Oxa-6-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-a-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, dihydrate, (2R,3S,4R,5R,8R,10R;1-Oxa-6-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-a-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, dihydrate, [2R-(2R*,3S*,4R*,5R*,8R*,10R*,11R*,12S*,13S*,14R*)]-;azithromycin hydrate;Azithromycin, CP 62993;CS-1348
CAS号:
117772-70-0
分子式:
C38H72N2O12
分子量:
748.99
EINECS号:
641-134-5
相关类别:
医药原料;抗生素;小分子抑制剂，天然产物;小分子抑制剂;药物杂质及中间体;原料药;化工原料;Macrolides (Antibiotics for Research and Experimental Use);Antibiotics for Research and Experimental Use;Biochemistry;Carbohydrates Derivatives;Chiral Reagents;Intermediates Fine Chemicals;Pfizer compounds;Pharmaceuticals;SELDANE;Inhibitors
Mol文件:
117772-70-0.mol
熔点
126 C
比旋光度
D26 -41.4° (c = 1 in CHCl3)
沸点
717℃
折射率
-47 ° (C=2, EtOH)
RTECS号
RN6960000
闪点
>110°(230°F)
储存条件
room temp
溶解度
Soluble in DMSO at 20mg/ml. Also soluble in chloroform or ethylene chloride
形态
powder
颜色
off-white
敏感性
Air Sensitive
Merck
14,915
EPA化学物质信息
1-Oxa-6-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-?-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-?-D-xylo-hexopyranosyl]oxy]-, dihydrate, (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)- (117772-70-0)
生物活性
Azithromycin Dihydrate 是对酸稳定的，口服的，大环内酯类抗菌药物，结构与红霉素相关。
体外研究
Azithromycin显示抗一系列相似谱的菌体活性。Azithromycin体外作用于革兰氏阳性菌其活性略低于红霉素，随着易感浓度下降到组织Azithromycin的浓度范围内，尽管这在临床意义上不确定。Azithromycin对红霉素的易感/ βL-ve 株, Streptococcus 株和 NS (非选择性抗敏感菌)/的平均MIC90分别为0.63, 0.35, 和<0.27 mg/L。相比之下，Azithromycin作用于大多革兰阴性菌和其他一些病原体的活性似乎比红霉素更强，特别是 Haemophilus influenza (MIC90, 1.34 mg/L), H. parainfluenzae (MIC90, 1 mg/L), Moraxella catarrhalis (MIC90, <0.1 mg/L), Neisseria gonorrhoeae (MIC90, 0.25 mg/L), Ureaplasma urealyticum , Bordetella spp (MIC90, 0.03-0.24 mg/L) 和 Borrelia burgdorferi 。Azithromycin也抗临床分离株厌氧革兰氏阳性菌 cocci 和 propionibacterium acnes 的活性，其MIC90为 2.3, 0.03 mg/L。像红霉素和其他大分子霉素一样，Azithromycin的活性不受β-内酰胺酶产生的影响。然而，红霉素耐药菌也耐Azithromycin。
体内研究
Azithromycin (50 mg/kg) has no effect on bronchoalveolar lavage inflammatory parameters and LDH levels in a mouse model of asthma exacerbation. Azithromycin induces neither general inflammatory parameters nor LDH release in a mouse model of asthma exacerbation, and augments expression of interferon-stimulated genes and the pattern recognition receptor MDA5 but not RIG-I in exacerbating mice.
用途
用于呼吸道感染、尿路感染、皮肤及软组织感染和性传播疾病
危险品标志
Xi
危险类别码
36/37/38
安全说明
24/25-36/37/39
WGK Germany
3
海关编码
29419000
