Moxifloxacin HCl Chemical Structure

Moxifloxacin HCl Chemical Structure
Molecular Weight: 437.89

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Moxifloxacin HCl is available in the following compound libraries:

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Product Description

Biological Activity

Description Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.
Targets Topoisomerase II [1] Topoisomerase IV [1]
In vitro Moxifloxacin exerts its effects by trapping a DNA drug enzyme complex and specifically inhibiting ATP-dependent enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. Moxifloxacin shows in-vitro potency against M. tuberculosis H37Rv with MIC of 0.177 μg/mL. Moxifloxacin has broad Grampositive and Gram-negative activity. Moxifloxacin shows in vitro and clinical efficacy against Staphylococcus aureus, Streptococcus pneumoniae, Str. pyogenes, Haemophilus influenzae, H. parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae and Mycoplasma pneumoniae. Moxifloxacin has activity against mycobacteria in addition to M. tuberculosis; Moxifloxacin is more active against M. kansasii than M. avium complex: specifically MIC90 for M. avium > M. intracellulare > M. kansasii at 4, 2 and 2 μg/mL, respectively. MIC90 for M. chelonae > M. fortuitum at 16 and 0.5 μg/mL, respectively. [1]
In vivo Moxifloxacin combined with RIF/pyrazinamide (PZA) reduces treatment time by up to 2 months compared to regimens with isoniazid (INH)/RIF/PZA in a mouse model designed to mimic human disease. Similar results with a stable cure are reached after 4 months in mice treated twice weekly with RIF/Moxifloxacin/PZA compared to cure in 6 months when daily treated with RIF/INH/PZA. 100 mg/kg Moxifloxacin in mice gives activity comparable to INH; increased dose in mice to 400 mg/kg Moxifloxacin daily results in spleen CFU counts lower than for INH 25 mg/kg although the differences are not statistically significant. AUC/MIC ratio correlates best with in-vivo efficacy for the fluoroquinolones in a mouse model of tuberculosis. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tuberculosis (Edinb), 2008, 88(2):127-131.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-08-21)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02236078 Not yet recruiting Tuberculosis|Drug-resistant Tuberculosis|Multidrug-resistant Tuberculosis Centers for Disease Control and Prevention|Kenya Medical  ...more Centers for Disease Control and Prevention|Kenya Medical Research Institute September 2015 --
NCT02515864 Not yet recruiting Healthy Fuji Yakuhin Co., Ltd. August 2015 Phase 2
NCT02409290 Not yet recruiting MDR-TB IUATLD, Inc|Medical Research Council July 2015 Phase 3
NCT01589497 Recruiting Tuberculosis AIDS Clinical Trials Group|National Institute of Allergy  ...more AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) June 2015 Phase 2
NCT02410772 Not yet recruiting Tuberculosis Centers for Disease Control and Prevention|AIDS Clinical  ...more Centers for Disease Control and Prevention|AIDS Clinical Trials Group June 2015 Phase 3

view more

Chemical Information

Download Moxifloxacin HCl SDF
Molecular Weight (MW) 437.89
Formula

C21H24FN3O4.HCl

CAS No. 186826-86-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms BAY12-8039 HCl
Solubility (25°C) * In vitro DMSO 88 mg/mL (200.96 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1-cyclopropyl-6-fluoro-8-methoxy-7-((4aS,7aS)-octahydropyrrolo[3,4-b]pyridin-6-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride

Product Use Citation (1)

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