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/ Levofloxacin/左氧氟沙星

Levofloxacin/左氧氟沙星 {[allProObj[0].p_purity_real_show]}

货号：A105051 同义名： (-)-Ofloxacin; MP-376

Levofloxacin 是一种 II 型拓扑异构酶抑制剂，能够抑制 DNA 回旋酶和拓扑异构酶 IV，IC50 分别为 8.06 µg/ml 和 9.81 µg/ml。Levofloxacin也具有抗菌活性。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Levofloxacin/左氧氟沙星 化学结构 CAS号：100986-85-4
Levofloxacin/左氧氟沙星 化学结构
CAS号：100986-85-4
Levofloxacin/左氧氟沙星 3D分子结构
CAS号：100986-85-4
Levofloxacin/左氧氟沙星 化学结构 CAS号：100986-85-4
Levofloxacin/左氧氟沙星 3D分子结构 CAS号：100986-85-4
规格 价格 会员价 库存 数量
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Levofloxacin/左氧氟沙星 纯度/质量文件 产品仅供科研

货号：A105051 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Topo I ↓ Topo II ↓ Topo IV ↓ Topoisomerase ↓ 其他靶点 纯度
Ellagic acid ✔ 98%
β-Lapachone ✔ 99%+
(s)-10-hydroxycamptothecin ✔ 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

 		98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

 		98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

 		98%
Irinotecan HCl Trihydrate ✔ 98%
SN-38 ✔ 98%
Levofloxacin hydrate ✔ 98%
Dexrazoxane ✔ 99%+
Ofloxacin ✔ 98+%
Enoxacin ✔ 99%+
Flumequine +

Topo II, IC50: 15 μM

 		98%
Levofloxacin ✔ 97%
Etoposide ✔ 98%
Pefloxacin mesylate dihydrate ✔ 99.5%
Marbofloxacin ✔ 98+%
Voreloxin HCl ✔ 98%
Mitoxantrone 2HCl ✔ PKC 98%
Nalidixic acid ✔ 98%
Doxorubicin ✔ 97%
Novobiocin sodium ✔ 95%
Amonafide ✔ 99%+
Pirarubicin ✔ 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

 		99%+
Genistein ✔ EGFR 98%
Teniposide ✔ 98%
Moxifloxacin ✔ 98%
Ciprofloxacin ✔ 98%
Clinafloxacin ✔ 99%
Gatifloxacin ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Epirubicin HCl ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Levofloxacin/左氧氟沙星 生物活性

靶点

  • Topo II
描述 Levofloxacin is a new fluoroquinolone antibiotic which is the active isomer of ofloxacin[3]. It is active against S. aureus, S. epidermidis, B. subtilis, E. coli, P. aeruginosa, and K. pneumoniae (MICs = 0.25, 0.25, 0.5, 0.03, 4, and 0.25 μg/ml, respectively)[4]. In stable chronic obstructive pulmonary disease, levofloxacin treatment (500mg/day) causes a short term reduction in bacterial load among patients[5].

Levofloxacin/左氧氟沙星 细胞实验

Cell Line
Concentration Treated Time Description References
Primary microglial cells 50-150 μg/ml 6 hours To investigate the inhibitory effect of levofloxacin on LPS-induced inflammatory response, results showed that levofloxacin significantly inhibited the release of IL-1β and TNF-α J Neuroinflammation. 2019 Jul 18;16(1):148.
Peritoneal macrophages 4 µg/mL 6, 12 h To evaluate the accumulation of levofloxacin in peritoneal macrophages. Results showed that 20(S)-Rh2 significantly increased the accumulation of levofloxacin in peritoneal macrophages in a concentration- and time-dependent manner. Acta Pharmacol Sin. 2021 Nov;42(11):1930-1941.
THP-1 macrophages 4, 8, 16 µg/mL 0.5, 1, 3, 6 h To evaluate the intracellular antibacterial activity of levofloxacin in THP-1 macrophages. Results showed that 20(S)-Rh2 significantly enhanced the bactericidal effect of levofloxacin against intracellular S. aureus in a concentration- and time-dependent manner. Acta Pharmacol Sin. 2021 Nov;42(11):1930-1941.

Levofloxacin/左氧氟沙星 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
ICR (CD-1) mice S. aureus 25923-induced peritonitis model Levofloxacin intravenous injection, 20(S)-Rh2 oral administration 1.5 mg/kg Single dose, observed for 24 hours To evaluate the therapeutic effect of levofloxacin combined with 20(S)-Rh2 in an infected mouse model. Results showed that the combination therapy significantly improved the survival rate of mice and reduced bacterial counts in peritoneal macrophages. Acta Pharmacol Sin. 2021 Nov;42(11):1930-1941.
Mice Murine model of K. pneumoniae lung infection Intraperitoneal injection 10 mg/kg or 50 mg/kg Single dose Evaluate the in vivo efficacy of BDM91288 combined with levofloxacin, results showed BDM91288 significantly enhanced the bactericidal effect of levofloxacin EMBO Mol Med. 2024 Jan;16(1):93-111
BALB/c mice Tuberculosis model Oral 300 mg/kg 5 days per week for 5 months To compare the efficacy of high-dose levofloxacin with moxifloxacin in tuberculosis treatment. Results showed that although initial bactericidal activity was similar, moxifloxacin demonstrated superior bactericidal activity during the continuation phase. Am J Respir Crit Care Med. 2013 Jul 1;188(1):97-102

Levofloxacin/左氧氟沙星 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00020865 Fever, Sweats, and Hot Flashes... 展开 >> Infection Leukemia Lymphoma Neutropenia Unspecified Adult Solid Tumor, Protocol Specific 收起 << Phase 3 Unknown - United States, California ... 展开 >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095-1781 收起 <<
NCT01131026 Helicobacter Pylori Infection Phase 3 Completed - Turkey ... 展开 >> Erciyes University School of Medicine Hospital, Department of Internal Medicine and Gastroenterology Kayseri, Turkey, 38039 收起 <<
NCT02975570 Tuberculosis Multi Drug Resist... 展开 >>ant Active 收起 << Phase 3 Withdrawn(The study could not ... 展开 >>be conducted since funding was not obtained.) 收起 << August 2022 -

Levofloxacin/左氧氟沙星 参考文献

[1]Davis R, Bryson HM. Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy. Drugs. 1994 Apr;47(4):677-700.

[2]Fu KP, Lafredo SC, et al. In vitro and in vivo antibacterial activities of levofloxacin (l-ofloxacin), an optically active ofloxacin. Antimicrob Agents Chemother. 1992 Apr;36(4):860-6.

[3]S Ragnar Norrby. Levofloxacin. Expert Opinion on Pharmacotherapy. 1999;1(1): 109-119.

[4]Mohammadhosseini N, Alipanahi Z, Alipour E, et al. Synthesis and antibacterial activity of novel levofloxacin derivatives containing a substituted thienylethyl moiety. Daru. 2012;20(1):16.

[5]Siva R, Bafadhel M, Monteiro W, Brightling CE, Pavord ID. Effect of levofloxacin on neutrophilic airway inflammation in stable COPD: a randomized, double-blind, placebo-controlled trial. Int J Chron Obstruct Pulmon Dis. 2014;9:179-186.

Levofloxacin/左氧氟沙星 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.84mL

2.77mL

1.38mL

27.67mL

5.53mL

2.77mL

Levofloxacin/左氧氟沙星 技术信息

CAS号100986-85-4
分子式C18H20FN3O4
分子量 361.37
SMILES Code O=C(C1=CN2C3=C(C=C(F)C(N4CCN(C)CC4)=C3OC[C@@H]2C)C1=O)O
MDL No. MFCD00865049
别名 (-)-Ofloxacin; MP-376; Levofloxacin, Levaquin, Tavanic, Iquix, Quixin; Fluoroquinolone
运输蓝冰
InChI Key GSDSWSVVBLHKDQ-JTQLQIEISA-N
Pubchem ID 149096
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

DMSO: 9 mg/mL(24.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(13.84 mM)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

Tags: Levofloxacin | (-)-Ofloxacin;MP-376;Levofloxacin, Levaquin, Tavanic, Iquix, Quixin;Fluoroquinolone | Quinolone | Topoisomerase | Antibacterial | AmBeed-信号通路专用抑制剂 | Levofloxacin/左氧氟沙星 纯度/质量文件 | Levofloxacin/左氧氟沙星 亚型比较 | Levofloxacin/左氧氟沙星 生物活性 | Levofloxacin/左氧氟沙星 临床数据 | Levofloxacin/左氧氟沙星 参考文献 | Levofloxacin/左氧氟沙星 实验方案 | Levofloxacin/左氧氟沙星 技术信息

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