1. Materials information
Names
| Name | 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid sesquihydrate |
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| Synonym | More Synonyms |
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Gatifloxacin sesquihydrate Biological Activity
| Description | Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate 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)[1]. Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo. |
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| Related Catalog | Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase Research Areas >> Infection Research Areas >> Inflammation/Immunology Signaling Pathways >> Anti-infection >> Bacterial |
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| Target | Topoisomerase II:36.7 μM (IC50) |
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| In Vitro | Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively[1]. Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively[1]. Gatifloxacin sesquihydrate exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin sesquihydrate displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935[2]. Gatifloxacin sesquihydrate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)[2]. Gatifloxacin sesquihydrate (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM Gatifloxacin sesquihydrate, respectively[3]. |
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| In Vivo | Gatifloxacin sesquihydrate (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis[4]. Animal Model: Female BALB/c mice with Nocardia brasiliensis in the right hind footpad[4] Dosage: 100 mg/kg Administration: Subcutaneous injection; 3 times a day; 30 days Result: Reduced the production of lesions in mice. |
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| References | [1]. Takei M, et al. Inhibitory activities of Gatifloxacin mesylate (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.Antimicrob Agents Chemother. 1998 Oct;42(10):2678-81. [2]. Fukuda H, et al. Antibacterial activity of Gatifloxacin mesylate (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [3]. Yamada C, et al. Gatifloxacin mesylate acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis. Eur J Pharmacol. 2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28. [4]. Daw-Garza A, et al. In vivo therapeutic effect of Gatifloxacin mesylate on BALB/c mice infected with Nocardia brasiliensis.Antimicrob Agents Chemother. 2008 Apr;52(4):1549-50. |
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Chemical & Physical Properties
| Density | 1.386 g/cm3 |
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| Boiling Point | 607.8ºC at 760 mmHg |
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| Molecular Formula | C19H22FN3O4.3/2H2O |
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| Molecular Weight | 804.834 |
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| Flash Point | 321.4ºC |
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| Exact Mass | 804.350586 |
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| PSA | 195.29000 |
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| LogP | 4.55550 |
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| Vapour Pressure | 6.43E-23mmHg at 25°C |
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MSDS
Gatifloxacin sesquihydrate MSDS(Chinese) |
Safety Information
| Symbol | 
GHS07 |
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| Signal Word | Warning |
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| Hazard Statements | H302 + H312 + H332 |
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| Precautionary Statements | P261-P280-P301 + P312 + P330 |
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| Hazard Codes | Xn |
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| Risk Phrases | 20/21/22 |
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| Safety Phrases | 36/37 |
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| RIDADR | NONH for all modes of transport |
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| HS Code | 2933990090 |
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Customs
| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
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