180200-66-2
180200-66-2 結(jié)構(gòu)式
基本信息
水合加替沙星
加替沙星水合物
加替沙星羧酸乙酯
加替沙星 USP標(biāo)準(zhǔn)品
1-環(huán)丙基-6-氟-4-氧代-8-甲氧基-7-(3-甲基
1-環(huán)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-環(huán)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-環(huán)丙基-6-氟-8-甲氧基-7-(3-甲基-1- 哌嗪)-4-氧代-喹啉-3-羧酸
1-環(huán)丙基-6-氟-8-甲氧基-7-(3-甲基哌嗪-1-基)-4-氧代-1,4-二氫3-喹啉羧酸
(+-)-1-C
AKOS NCG1-0010
Gatifloxacin Tablet
Gatifloxacin (300 mg)
Gatifloxacin Monohydrate
Gatifloxacin sesquihydrate
Gatifloxacin formic acid ethyl ester
Gatifloxacin sesquihydrate USP/EP/BP
Gatifloxacin sesquihydrate Micronized
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
Acute Tox. 4 Inhalation
Acute Tox. 4 Oral
常見問題列表
水合加替沙星是一種口服氟喹諾酮類廣譜抗生素，通過抑制細(xì)菌的DNA旋轉(zhuǎn)酶和拓?fù)洚悩?gòu)酶IV發(fā)揮作用，并增強(qiáng)了對(duì)革蘭氏陽性菌及厭氧菌的抗菌活性。
水合加替沙星可用于治療眼部感染，且未見引起光毒性反應(yīng)。
水合加替沙星(AM-1155 sesquihydrate) 是一種有效的氟喹諾酮類抗生素 (antibiotic)，具有廣譜抗菌活性。其可抑制細(xì)菌 II 型拓?fù)洚悩?gòu)酶 (type II topoisomerases) (IC50=13.8 μg/ml; 金黃色葡萄球菌拓?fù)洚悩?gòu)酶 IV) 和大腸桿菌 DNA 解旋酶 (IC50=0.109 μg/ml)。其在動(dòng)物模型中，可用于細(xì)菌性結(jié)膜炎的研究。
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Topoisomerase II 36.7 μM (IC 50 ) |
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.
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. |