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Levofloxacin hydrate

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Chemical Structure| 138199-71-0 同义名 : 左氧氟沙星半水合物 ;Levofloxacin hemihydrate;Levaquin hydrate;Cravit hydrate;Iquix hydrate;Quixin hydrate;Tavanic hydrate
CAS号 : 138199-71-0
货号 : A126121
分子式 : C36H42F2N6O9
纯度 : 98%
分子量 : 740.75
MDL号 : MFCD07772024
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(9.45 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: 50 mg/mL(67.5 mM)
动物实验配方：
生物活性
靶点

  • Topo II
描述 Levofloxacin (Hemihydrate) is a fluoroquinolone antibiotic and is the optical S-(-) isomer of the racemic drug substance ofloxacin. It has a broad spectrum of in vitro activity against Gram-positive and Gram-negative bacteria, as well as certain other pathogens such as Mycoplasma, Chlamydia, Legionella and Mycobacteria spp. Plasma concentrations in healthy volunteers reach a mean peak drug plasma concentration (Cmax) of approximately 2.8 and 5.2 mg/L within 1 to 2 hours after oral administration of levofloxacin 250 and 500 mg tablets, respectively[3]. In stable COPD (chronic obstructive pulmonary disease), levofloxacin treatment causes a short-term reduction in bacterial load[4]. Levofloxacin was found to significantly improve the clinical and microbiological parameters in CP (chronic periodontitis) individuals[5]. A 30-day course of levofloxacin does not significantly improve BK viral load reduction or allograft function when used in addition to overall reduction of immunosuppression[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.35mL

0.27mL

0.14mL

6.75mL

1.35mL

0.68mL

13.50mL

2.70mL

1.35mL
参考文献

[1]Mourelle-Insua A, Lopez-Iglesias M, et al.Stereoselective Access to 1-[2-Bromo(het)aryloxy] propan-2-amines Using Transaminases and Lipases; Development of a Chemoenzymatic Strategy Toward a Levofloxacin Precursor. J Org Chem. 2016 Oct 21;81(20):9765-9774.

[2]Mori K, Maru C, Takasuna K. Characterization of histamine release induced by fluoroquinolone antibacterial agents in-vivo and in-vitro. J Pharm Pharmacol. 2000 May;52(5):577-84.

[3]Fish DN, Chow AT. The clinical pharmacokinetics of levofloxacin. Clin Pharmacokinet. 1997;32(2):101–119

[4]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.

[5]Pradeep AR, Singh SP, Martande SS, et al. Clinical and microbiological effects of levofloxacin in the treatment of chronic periodontitis: a randomized, placebo-controlled clinical trial. J Investig Clin Dent. 2015;6(3):170–178

[6]Lee BT, Gabardi S, Grafals M, et al. Efficacy of levofloxacin in the treatment of BK viremia: a multicenter, double-blinded, randomized, placebo-controlled trial. Clin J Am Soc Nephrol. 2014;9(3):583–589