| Size | Price | Stock | Qty |
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| 500mg |
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| 10g |
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Purity: ≥98%
Gatifloxacin (formerly also known as AM-1155, CG5501, BMS-206584; PD135432; Tequin; Zymar; Gatiflo; Zymaxid; AM 1155) is a fourth-generation antibiotic of the fluoroquinolone family used to treat tuberculosis and pneumonia, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Both gatifloxacin and moxifloxacin are significantly more active than levofloxacin and have somewhat better in vitro activity against M. tuberculosis. Gatifloxacin has MICs of 0.125 μg/mL against M. tuberculosis ATCC 35801. Among the quinolones tested, gatifloxacin has the lowest activity against HeLa cell topoisomerase II (IC50 = 265 mg/mL), despite having strong inhibitory effects against bacterial type II topoisomerases.
| Targets |
Topoisomerase II ( IC50 = 36.7 μM ); Quinolone
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The bacterial enzymes DNA gyrase and topoisomerase IV are inhibited by the antibiotic gatifloxacin, which belongs to the fourth generation fluoroquinolone family.
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| Cell Assay |
Antimicrobial Like other members of the fourth-generation fluoroquinolone family of antibiotics, gatifloxacin inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. When it came to the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), gatifloxacin exhibited activity comparable to that of tosufloxacin and more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin. These results suggest that gatifloxacin has the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones studied. In the case of Pseudomonas aeruginosa-infected corneal ulcers, ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin when given less frequently. Fluorescein retention scores showed a trend favoring gatifloxacin.
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| Animal Protocol |
Female BALB/c mice with Nocardia brasiliensis in the right hind footpad
100 mg/kg Subcutaneous injection; 3 times a day; 30 days |
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| References |
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| Molecular Formula |
C19H22FN3O4
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| Molecular Weight |
375.39
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| Exact Mass |
375.4
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| Elemental Analysis |
C, 60.79; H, 5.91; F, 5.06; N, 11.19; O, 17.05
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| CAS # |
112811-59-3
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| Related CAS # |
121577-32-0；316819-28-0；180200-66-2
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| Appearance |
Solid powder
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| SMILES |
CC1CN(CCN1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F
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| InChi Key |
XUBOMFCQGDBHNK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22FN3O4/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)
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| Chemical Name |
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6639 mL | 13.3195 mL | 26.6390 mL | |
| 5 mM | 0.5328 mL | 2.6639 mL | 5.3278 mL | |
| 10 mM | 0.2664 mL | 1.3319 mL | 2.6639 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00905762 | Completed | Drug: Gatifloxacin Drug: Moxifloxacin |
Healthy | Bausch & Lomb Incorporated | March 2009 | Phase 1 |
| NCT00410891 | Completed | Drug: gatifloxacin | Intravitreous Injections |
Stanford University | July 2008 | Phase 4 |
| NCT00464438 | Completed | Drug: moxifloxacin 0.5% eye drops Drug: gatifloxacin |
Bacterial Conjunctivitis | Allergan | June 2007 | Phase 4 |
| NCT00414011 | Completed | Drug: Moxifloxacin Drug: Gatifloxacin |
Epithelium, Corneal | Walter Reed Army Medical Center | February 2005 | Not Applicable |
| NCT00396084 | Completed | Drug: Gatifloxacin Drug: Isoniazid |
Tuberculosis | National Institute of Allergy and Infectious Diseases (NIAID) |
February 10, 2004 | Phase 1 Phase 2 |
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