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

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

目錄號(hào): HY-10581 純度: 99.55%
COA 產(chǎn)品使用指南

Gatifloxacin (AM-1155) 是一種有效的氟喹諾酮類抗生素 (antibiotic)，具有廣譜抗菌活性。Gatifloxacin 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)。Gatifloxacin 在動(dòng)物模型中具有抗細(xì)菌性結(jié)膜炎作用。

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Gatifloxacin Chemical Structure

Gatifloxacin Chemical Structure

CAS No. : 112811-59-3

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500 mg ￥400
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5 g ￥980
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Customer Review

Other Forms of Gatifloxacin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)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]
體外研究
(In Vitro)

Gatifloxacin 抗金黃色葡萄球菌 MS5935 拓?fù)洚悩?gòu)酶 IV，E. coli NIHJ JC-2 DNA gyrase 和 HeLa 細(xì)胞拓?fù)洚悩?gòu)酶 II 的 IC50 值分別為 13.8 μg/mL、0.109 μg/mL 和 265 μg/mL[1]。
Gatifloxacin 對(duì) S.金黃色葡萄球菌 的 MS5935 拓?fù)洚悩?gòu)酶 IV，E.大腸桿菌 NIHJ JC-2 DNA 促旋酶和 HeLa 細(xì)胞拓?fù)洚悩?gòu)酶II的 MIC 值分別為 0.05 μg/mL、0.0063 μg/mL和122 μg/mL[1]。
Gatifloxacin 對(duì)野生型菌株 (MS5935、MS5952、MR5867 和 MR6009) 以及第一步、第二步、第三步和第四步突變體具有抗菌活性，MIC 值為 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 的第二步突變體外，Gatifloxacin 對(duì)第二步和第三步突變體 (MS5952、MR5867和MR6009) 表現(xiàn)出最強(qiáng)的活性，對(duì) norA 轉(zhuǎn)化體 NY12 的活性 (MIC，0.39 μg/mL)[2]。
Gatifloxacin (20-100 μM；72 小時(shí)) 在第 1 天顯著降低胰島素含量至 60%，并且在第 3 天，20 μM 和 100 μM 加替沙星分別繼續(xù)降低至 50.1% 和 44.7%[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Gatifloxacin (皮下注射；100 mg/kg；每天 3 次；30 天) 顯著減少巴西諾卡氏菌小鼠足墊的病變數(shù)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

加替沙星
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, stored under nitrogen

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 2 mg/mL (5.33 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : 1 mg/mL (2.66 mM; 超聲助溶)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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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Gatifloxacin
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