Gatifloxacin hydrochloride

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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:

121577-32-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
500mg	电议
1 g	电议
5 g	电议
10 g	电议
50 g	电议

产品名称

加替沙星盐酸盐
AM-1155 hydrochloride
BMS-206584 hydrochloride
PD135432 hydrochloride

产品介绍

Gatifloxacin hydrochloride (AM-1155 hydrochloride) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。Gatifloxacin hydrochloride (AM-1155 hydrochloride) 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 hydrochloride (AM-1155 hydrochloride) 在动物模型中，可用于细菌性结膜炎的研究。

生物活性

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

IC₅₀& Target^[1]

Quinolone

Topoisomerase II

36.7 μM ()

体外研究
(In Vitro)

Gatifloxacin hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)^[2].
Gatifloxacin hydrochloride (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 hydrochloride, respectively^[3].

体内研究
(In Vivo)

Gatifloxacin hydrochloride (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^[1]
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

411.86

性状

Solid

Formula

C₁₉H₂₃ClFN₃O₄

CAS 号

121577-32-0

中文名称

加替沙星盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 10 mg/mL(24.28 mM;Need ultrasonic)

DMSO : 4 mg/mL(9.71 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4280 mL	12.1400 mL	24.2801 mL
5 mM	0.4856 mL	2.4280 mL	4.8560 mL
10 mM	0.2428 mL	1.2140 mL	2.4280 mL

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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 6.67 mg/mL (16.19 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。