Gatifloxacin

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Gatifloxacin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

112811-59-3

包装与价格：

包装	价格(元)
500mg	电议
1 g	电议
5 g	电议
10 g	电议
50 g	电议

产品名称

加替沙星
AM-1155
BMS-206584
PD135432

产品介绍

Gatifloxacin (AM-1155) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。Gatifloxacin 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 在动物模型中具有抗细菌性结膜炎作用。

生物活性

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinoloneantibioticwith broad-spectrum antibacterial activity. Gatifloxacin inhibitsbacterialtype II topoisomerases(IC₅₀=13.8 μg/ml forS. aureustopoisomeraseIV) andE. coliDNA gyrase(IC₅₀=0.109 μg/ml)^[1]. Gatifloxacin can be used to treatbacterialconjunctivitis in vivo.

IC₅₀& Target^[1]

Quinolone

Topoisomerase II

36.7 μM (IC₅₀)

体外研究
(In Vitro)

Gatifloxacin is againstS. aureus MS5935 topoisomerase IV,E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC₅₀values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively^[1].
Gatifloxacin is againstS. 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^[1].
Gatifloxacin 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 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^[2].
Gatifloxacin has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)^[2].
Gatifloxacin (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, respectively^[3].

体内研究
(In Vivo)

Gatifloxacin (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad withNocardia brasiliensis^[4].

Animal Model:	Female BALB/c mice withNocardia brasiliensisin 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.

Clinical Trial

分子量

375.39

性状

Solid

Formula

C₁₉H₂₂FN₃O₄

CAS 号

112811-59-3

中文名称

加替沙星

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 2 mg/mL(5.33 mM;Need ultrasonic)

H₂O : 1 mg/mL(2.66 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.6639 mL	13.3195 mL	26.6390 mL
5 mM	0.5328 mL	2.6639 mL	5.3278 mL
10 mM	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。