水合加替沙星

中文名称:

水合加替沙星

中文同义词:

1-环丙基-6-氟-4-氧代-8-甲氧基-7-(3-甲基;1-环丙基-6-氟-8-甲氧基-7-(3-甲基-1- 哌嗪)-4-氧代-喹啉-3-羧酸;1-环丙基-6-氟-8-甲氧基-7-(3-甲基哌嗪-1-基)-4-氧代-1,4-二氢3-喹啉羧酸;1-环丙基-6-氟-8-甲氧基-7-(3-甲基哌嗪-1-基)-4-氧代-3-喹啉羧酸;1-环丙基-6-氟-8-甲氧基-7-(3-甲基哌嗪-1-基)-4-氧代3-喹啉羧酸;加替沙星羧酸乙酯;加替沙星水合物;水合加替沙星

英文名称:

Gatifloxacin sesquihydrate

英文同义词:

Gatifloxacin formic acid ethyl ester;Gatifloxacin (300 mg);Gatifloxacin Monohydrate;Gatifloxcin 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid;3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-, hydrate (2:3);(+-)-1-C;1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid;1-Cyclopropyl-6-fluoro-8-Methoxy-7-(3-Methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid sesquihydrate

CAS号:

180200-66-2

分子式:

C19H24FN3O5

分子量:

393.42

EINECS号:

672-577-2

相关类别:

喹诺酮类;医用原料;医药原料;医药原料药;原料药;原料;Active Pharmaceutical Ingredients;APIs;医药原料;化工原料

Mol文件:

180200-66-2.mol

沸点

684℃

RTECS号

VB1983600

储存条件

Keep in dark place,Inert atmosphere,2-8°C

溶解度

Soluble in 1N NaOH at 10mg/ml

形态

neat

BRN

14390028

生物活性

Gatifloxacin sesquihydrate (AM-1155 sesquihydrate) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。Gatifloxacin sesquihydrate (AM-1155 sesquihydrate) 可抑制细菌 II 型拓扑异构酶 (type II topoisomerases) (IC50=13.8 μg/ml; 金黄色葡萄球菌拓扑异构酶 IV) 和大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)。Gatifloxacin sesquihydrate (AM-1155 sesquihydrate) 在动物模型中，可用于细菌性结膜炎的研究。

靶点

Topoisomerase II 36.7 μM (IC 50 )

体外研究

Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC 50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively.Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively.Gatifloxacin sesquihydrate exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin sesquihydrate displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935.Gatifloxacin sesquihydrate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml).Gatifloxacin sesquihydrate (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM Gatifloxacin sesquihydrate, respectively.

体内研究

Gatifloxacin sesquihydrate (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis . Animal Model: Female BALB/c mice with Nocardia brasiliensis in the right hind footpad Dosage: 100 mg/kg Administration: Subcutaneous injection; 3 times a day; 30 days Result: Reduced the production of lesions in mice.

Animal Model:

Female BALB/c mice with Nocardia brasiliensis in the right hind footpad

Dosage:

100 mg/kg

Administration:

Subcutaneous injection; 3 times a day; 30 days

Result:

Reduced the production of lesions in mice.

危险品标志

危险类别码

20/21/22

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