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Gatifloxacin hydrochloride

CAS# 121577-32-0

Gatifloxacin hydrochloride

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Quality Control of Gatifloxacin hydrochloride

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Chemical structure

Gatifloxacin hydrochloride

3D structure

Chemical Properties of Gatifloxacin hydrochloride

Cas No. 121577-32-0 SDF Download SDF
PubChem ID 17956339 Appearance Powder
Formula C19H23ClFN3O4 M.Wt 411.86
Type of Compound N/A Storage Desiccate at -20°C
Synonyms AM 1155 hydrochloride; BMS 206584-01 hydrochloride; PD 135432 hydrochloride
Solubility Soluble in DMSO
Chemical Name 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;hydrochloride
SMILES CC1CN(CCN1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F.Cl
Standard InChIKey GQYBNVXJQVIRGC-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H22FN3O4.ClH/c1-10-8-22(6-5-21-10)16-14(20)7-12-15(18(16)27-2)23(11-3-4-11)9-13(17(12)24)19(25)26;/h7,9-11,21H,3-6,8H2,1-2H3,(H,25,26);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Gatifloxacin hydrochloride

DescriptionGatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Target: Antibacterial Gatifloxacin (hydrochloride) is the hydrochloride salt of Gatifloxacin which is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1]. Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2]. Clinical indications: Bacterial infection FDA Approved Date: Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]

References:
[1]. Fukuda, H., S. Hori, and K. Hiramatsu, Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. A [2]. Jensen, H., et al., Comparison of ophthalmic gatifloxacin 0.3% and ciprofloxacin 0.3% in healing of corneal ulcers associated with Pseudomonas aeruginosa-induced ulcerative keratitis in rabbits. J Ocul Pharmacol Ther, 2005. 21(1): p. 36-43. [3]. Cheung, O., et al., Gatifloxacin-induced hepatotoxicity and acute pancreatitis. Ann Intern Med, 2004. 140(1): p. 73-4. [4]. Fteha, A., et al., Gatifloxacin induced torsades de pointes. Pacing Clin Electrophysiol, 2004. 27(10): p. 1449-50.

Gatifloxacin hydrochloride Dilution Calculator

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Gatifloxacin hydrochloride Molarity Calculator

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Preparing Stock Solutions of Gatifloxacin hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.428 mL 12.14 mL 24.2801 mL 48.5602 mL 60.7002 mL
5 mM 0.4856 mL 2.428 mL 4.856 mL 9.712 mL 12.14 mL
10 mM 0.2428 mL 1.214 mL 2.428 mL 4.856 mL 6.07 mL
50 mM 0.0486 mL 0.2428 mL 0.4856 mL 0.9712 mL 1.214 mL
100 mM 0.0243 mL 0.1214 mL 0.2428 mL 0.4856 mL 0.607 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Gatifloxacin hydrochloride

Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

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References on Gatifloxacin hydrochloride

Simultaneous determination of gatifloxacin and ambroxol hydrochloride from tablet dosage form using reversed-phase high performance liquid chromatography.[Pubmed:18724676]

Se Pu. 2008 May;26(3):358-61.

A reversed-phase high performance liquid chromatography (HPLC) method was developed, validated, and used for the quantitative determination of gatifloxacin (GA) and ambroxol hydrochloride (AM), from its tablet dosage form. Chromatographic separation was performed on a HiQ Sil C18 column (250 mm x 4.6 mm, 5 microm), with a mobile phase comprising of a mixture of 0.01 mol/L potassium dihydrogen orthophosphate buffer and acetonitrile (70 : 30, v/v), and pH adjusted to 3 with orthophosphoric acid, at a flow rate of 1 mL/min, with detection at 247 nm. Separation was completed in less than 10 min. As per International Conference on Harmonisation (ICH) guidelines the method was validated for linearity, accuracy, precision, limit of quantitation, limit of detection, and robustness. Linearity of GA was found to be in the range of 10 -60 microg/mL and that for AM was found to be 5 - 30 microg/mL. The correlation coefficients were 0.999 6 and 0.999 3 for GA and AM respectively. The results of the tablet analysis (n = 5) were found to be 99.94% with +/- 0.25% standard deviation (SD) and 99.98% with +/- 0.36% SD for GA and AM respectively. Percent recovery of GA was found to be 99.92% - 100.02% and that of AM was 99.86% - 100.16%. The assay experiment shows that the method is free from interference of excipients. This demonstrates that the developed HPLC method is simple, linear, precise, and accurate, and can be conveniently adopted for the routine quality control analysis of the tablet.

Evaluation of 0.3% gatifloxacin hydrochloride in decontamination of donor corneas.[Pubmed:22878383]

Eye Contact Lens. 2012 Sep;38(5):295-9.

PURPOSE: To evaluate demographic, clinical, and microbiological profile of eye donors and efficacy of 0.3% Gatifloxacin hydrochloride in microbial decontamination of donor corneas. METHODS: About 513 donors and 1,026 corneas received at National Eye Bank of a tertiary care hospital during 1-year period were analyzed prospectively in this randomized clinical trial. The donor eyes were graded and treated with 5% povidone-iodine, 0.4% amikacin sulphate, and 0.3% Gatifloxacin hydrochloride. The parameters evaluated were death enucleation time (DET), grading of donor corneas, microbiological profile of culture organisms, and their sensitivity to various antibiotics. RESULTS: Mean DET was 6.29+/-5.7 hours. Forty one percent eyes were optical grade corneas and the majority of donors (38.5%) had accidental deaths. Good grade eyes were maximum with DET of <1 hour and were comparable between 0-6 hours and 6-12 hours. About 57.6% (591/1026) eyes were culture positive; most common organisms were Pseudomonas spp (53%) and Coagulase-negative Staphylococci (24%). Culture positivity reduced significantly after treatment with povidone iodine and amikacin (P=0.002, right eye; P=0.004; left eye) and decreased further with use of gatifloxacin (P=0.001). Pseudomonas (93%), Coagulase-negative Staphylococci (96.3%), Staphylococcus aureus (90.5%), enterococci and gram-negative bacilli were sensitive to gatifloxacin. Pseudomonas spp which were multidrug-resistant were sensitive to polymyxin-B. CONCLUSIONS: Gatifloxacin hydrochloride in addition to amikacin sulphate is beneficial for donor eye decontamination. Polymyxin-B may be used for multidrug-resistant Pseudomonas spp.

Description

Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride 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). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.

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