1. Anti-infection Cell Cycle/DNA Damage
  2. Bacterial Topoisomerase Antibiotic
  3. Gatifloxacin mesylate

Gatifloxacin mesylate  (Synonyms: 甲磺酸加替沙星; AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate)

目录号: HY-10581B
产品使用指南

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

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Gatifloxacin mesylate Chemical Structure

Gatifloxacin mesylate Chemical Structure

CAS No. : 316819-28-0

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml)[1]. Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.

IC50 & Target[1]

Quinolone

 

Topoisomerase II

36.7 μM (IC50)

体外研究
(In Vitro)

Gatifloxacin mesylate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively[1].
Gatifloxacin mesylate 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[1].
Gatifloxacin mesylate 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 mesylate 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 mesylate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)[2].
Gatifloxacin mesylate (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 mesylate, respectively[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

471.50

Formula

C20H26FN3O7S

CAS 号
中文名称

甲磺酸加替沙星

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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