Gatifloxacin (Synonyms: 加替沙星; AM-1155; BMS-206584; PD135432)

目录号: HY-10581 纯度: 99.55%: FAQs
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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。

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Gatifloxacin Chemical Structure

CAS No. : 112811-59-3

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Customer Review

Other Forms of Gatifloxacin:

MCE 顾客使用本产品发表的 4 篇科研文献

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生物活性
纯度 & 产品资料
参考文献

生物活性

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin 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 can be used to treat bacterial conjunctivitis?in vivo.

IC₅₀ & Target^[1]

Quinolone

Topoisomerase II

36.7 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
MDCK	CC₅₀	396 μM Compound: GTFX	Cytotoxicity against MDCK cells after 48 hrs by CPE assay Cytotoxicity against MDCK cells after 48 hrs by CPE assay	[PMID: 21481984]
NIH3T3	IC₅₀	596 μM Compound: 5	Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 18950903]
T-cell	IC₅₀	> 50 μg/mL Compound: GTX	Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method	10.1007/s00044-009-9264-y
Vero	CC₅₀	> 155.3 μM Compound: Gati	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18502542]
Vero	IC₅₀	> 155.3 μM Compound: Gati	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18304818]
Vero	IC₅₀	> 155.3 μM Compound: gatifloxacin	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18078756]
Vero	IC₅₀	> 155.3 μM Compound: Gati	Cytotoxicity against Vero cells after 72 hrs by MTT assay Cytotoxicity against Vero cells after 72 hrs by MTT assay	[PMID: 17960928]
Vero	IC₅₀	> 159.5 μM Compound: Gatifloxacin	Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr	10.1007/s00044-010-9322-5
Vero	IC₅₀	> 550 μM Compound: Gatifloxacin	Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay	10.1007/s00044-011-9646-9
Vero	CC₅₀	125 μg/mL Compound: GTFX	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28720502]
Vero	CC₅₀	125 μg/mL Compound: GTFX	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28646656]
Vero	CC₅₀	64 μg/mL Compound: Gatifloxacin	Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay	[PMID: 31352245]

体外研究
(In Vitro)

Gatifloxacin 抗金黄色葡萄球菌 MS5935 拓扑异构酶 IV，E. coli NIHJ JC-2 DNA gyrase 和 HeLa 细胞拓扑异构酶 II 的 IC₅₀ 值分别为 13.8 μg/mL、0.109 μg/mL 和 265 μg/mL^[1]。
Gatifloxacin 对 S.金黄色葡萄球菌 的 MS5935 拓扑异构酶 IV，E.大肠杆菌 NIHJ JC-2 DNA 促旋酶和 HeLa 细胞拓扑异构酶II的 MIC 值分别为 0.05 μg/mL、0.0063 μg/mL和122 μg/mL^[1]。
Gatifloxacin 对野生型菌株 (MS5935、MS5952、MR5867 和 MR6009) 以及第一步、第二步、第三步和第四步突变体具有抗菌活性，MIC 值为 0.05 至 0.10 μg/mL，0.20 μg/mL、1.56 至 3.13 μg/mL、1.56 至 6.25 μg/mL 和 50 至 200 μg/mL。除菌株MS5935 的第二步突变体外，Gatifloxacin 对第二步和第三步突变体 (MS5952、MR5867和MR6009) 表现出最强的活性，对 norA 转化体 NY12 的活性 (MIC，0.39 μg/mL)^[2]。
Gatifloxacin (20-100 μM；72 小时) 在第 1 天显著降低胰岛素含量至 60%，并且在第 3 天，20 μM 和 100 μM 加替沙星分别继续降低至 50.1% 和 44.7%^[3]。

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

体内研究
(In Vivo)

Gatifloxacin (皮下注射；100 mg/kg；每天 3 次；30 天) 显著减少巴西诺卡氏菌小鼠足垫的病变数量^[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

375.39

Formula

C₁₉H₂₂FN₃O₄

CAS 号

112811-59-3

性状

固体

颜色

White to off-white

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

细胞实验：

DMSO 中的溶解度 : 2 mg/mL (5.33 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 1 mg/mL (2.66 mM; 超声助溶)

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	---	---	---

查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.55%

选择批次：

Data Sheet (623 KB) SDS (393 KB)

COA (287 KB) LCMS (264 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Takei M, et al. Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.Antimicrob Agents Chemother. 1998 Oct;42(10):2678-81. [Content Brief]

[2]. Fukuda H, et al. Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [Content Brief]

[3]. Yamada C, et al. Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis. Eur J Pharmacol. 2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28. [Content Brief]

Gatifloxacin 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.6639 mL	13.3195 mL	26.6390 mL	66.5974 mL
DMSO	5 mM	0.5328 mL	2.6639 mL	5.3278 mL	13.3195 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Gatifloxacin (Synonyms: 加替沙星; AM-1155; BMS-206584; PD135432)

Customer Review

Other Forms of Gatifloxacin:

MCE 顾客使用本产品发表的 4 篇科研文献