Gemifloxacin mesylate|210353-53-0|(甲磺酸吉米沙星; SB-265805S; LB-20304a)-陌孚医药/Medlife

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Gemifloxacin mesylate (Synonyms: 甲磺酸吉米沙星; SB-265805S; LB-20304a)

目录号: PL05450 纯度: ≥99%

CAS No. :210353-53-0

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中文名称	Gemifloxacin mesylate
中文别名	甲磺酸吉米沙星;7-[3-(氨甲基)-4-(甲氧亚氨基)吡咯烷-1-基]-1-环丙基-6-氟-4-氧代-1,4-二氢-1,8-二氮杂萘-3-羧酸甲磺酸盐;2-硝基-4-硫氰基苯胺
英文名称	Gemifloxacin mesylate
英文别名	Gemifioxacin mesylate;7-(3-Aminomethyl)-4-methoxyimino-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid mesylate;Gemifloxacin Mesilate;GEMIFLOXACIN MESYLATE;LB-20304a;SB-265805S;7-(4-Aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid mesylate;7-[(4Z)-3-(Aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid monomethanesulfonate;Factive;Gemifloxacin (mesylate);Gemifloxacin mesylate [USAN];DSSTox_CID_25948;DSSTox_RID_81245;DSSTox_GSID_45948;Gemifloxacin mesylate (USAN);LB 20304a;C18H20FN5O4.CH4O3O;Floxguard;Gemixa;1,8-Naphthyridine-3-carboxylic acid, 7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-, monome
Cas No.	210353-53-0
分子式	C₁₉H₂₄FN₅O₇S
分子量	485.49
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

Gemifloxacin mesylate (SB-265805S; LB-20304a) 是一种具有口服活性的广谱性喹诺酮类抗菌抗生素 (antibiotic)。Gemifloxacin mesylate 通过抑制 DNA 旋回酶 (DNA gyrase) 和拓扑异构酶 IV (Topoisomerase IV) 活性抑制DNA合成 (DNA synthesis)。Gemifloxacin mesylate 对革兰氏阳性菌有较强的体外抑菌活性，特别是链球菌 (Streptococci) 和葡萄球菌 (Staphylococci)。Gemifloxacin mesylate 已被用于呼吸道感染的研究。

生物活性

Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.

性状

Solid

IC50 & Target[1][2]

Antibiotic, Bacterial, DNA synthesis, Topoisomerase IV

体外研究(In Vitro)

Gemifloxacin has higher antibacterial activity than Moxifloxacin (HY-66011A) against Streptococcus pneumoniae with a MIC90 of 0.06 μg/mL.
Gemifloxacin has highly potent antibacterial activity against Penicillin-resistant strains of S. pneumoniae with a MIC90 of 0.03 μg/mL. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Gemifloxacin has favorable pharmacokinetic profile in animals after oral administration.
Pharmacokinetic Parameters of Gemifloxacin in Sprague-Dawley rats and dogs.
Species Administration AUC 0-24 (μg/mL·h)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Hong CY. Discovery of gemifloxacin (Factive, LB20304a): a quinolone of a new generation. Farmaco. 2001 Jan-Feb;56(1-2):41-4.
[2]. Allen A, Kim I, et al. Multiple-dose pharmacokinetics and tolerability of gemifloxacin administered orally to healthy volunteers. Antimicrob Agents Chemother. 2001 Feb;45(2):540-5.

溶解度数据	In Vitro: DMSO : 100 mg/mL (205.98 mM; Need ultrasonic)H₂O : 50 mg/mL (102.99 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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