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| ln Vitro |
Amifloxacin (WIN 49375) exhibits moderate activity against Staphylococcus aureus with a minimum inhibitory concentration (MIC) of less than or equal to 2 μg/mL and is active in vitro against isolates of Pseudomonas aeruginosa.
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| ln Vivo |
Amifloxacin (WIN 49375) has a 50% effective dose when taken orally, which is two to three times the parenteral dose. This makes it a very active medication. These experimental infections show that amifloxacin works well when taken in different ways. When amifloxacin was given subcutaneously, intravenously, or orally to mice infected intraperitoneally with E. coli Vogel 0.5 hours postinfection, the corresponding ED50 values were 0.6, 0.8, and 1.0 mg/kg [1]. Rats were given oral [14C]amifloxacin mesylate at a dose of 20 mg/kg, and 0.5 hours later, the blood radioactivity peaked at 7.1±0.26 μg amifloxacin per milliliter. Blood radioactivity dropped quickly from 7.0±0.25μg/mL to 1.2±0.12μg/mL between 0.75 and 4 hours. The decrease in blood radioactivity is more gradual and intricate between 8 and 48 hours. Blood radioactivity was equal to 0.14 ± 0.02 μg/mL after 48 hours. Blood radioactivity levels in rats dropped from 29.1 ± 0.85 μg/mL at 1.0 minutes to 14.4 ± 0.52 μg/mL at 10 minutes following an intravenous administration of 20 mg/kg [14C]amifloxacin mesylate. Blood radioactivity dropped log-linearly from 13.0±0.42 μg/mL to 0.97±0.09 μg/mL between 0.25 and 4 hours. Between 4 and 24 hours, elimination is more difficult and takes longer. Blood radioactivity is equal to 0.12±0.01 ug/mL after 24 hours[2].
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| References |
[1]. Cornett JB, et al. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin). Antimicrob Agents Chemother. 1985 Jan;27(1):4-10.
[2]. Johnson JA, et al. Metabolism and disposition of amifloxacin in laboratory animals. Antimicrob Agents Chemother. 1985 May;27(5):774-81 |
| Additional Infomation |
Amifloxacin is a member of quinolines.
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| Molecular Formula |
C16H19FN4O3
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|---|---|
| Molecular Weight |
334.3455
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| Exact Mass |
334.144
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| CAS # |
86393-37-5
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| Related CAS # |
88036-80-0 (mesylate);86393-37-5;
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| PubChem CID |
55492
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| Appearance |
White to light yellow solid powder
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| Density |
1.44g/cm3
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| Boiling Point |
532.5ºC at 760mmHg
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| Melting Point |
300 °C
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| Flash Point |
275.8ºC
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| Index of Refraction |
1.662
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| LogP |
0.839
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C(=O)C2C(=CC(N3CCN(C)CC3)=C(C=2)F)N(NC)C=1)O
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| InChi Key |
RUXPNBWPIRDVTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19FN4O3/c1-18-21-9-11(16(23)24)15(22)10-7-12(17)14(8-13(10)21)20-5-3-19(2)4-6-20/h7-9,18H,3-6H2,1-2H3,(H,23,24)
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| Chemical Name |
6-fluoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
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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 |
| 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) |
H2O : ~50 mg/mL (~149.54 mM)
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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 | 2.9909 mL | 14.9544 mL | 29.9088 mL | |
| 5 mM | 0.5982 mL | 2.9909 mL | 5.9818 mL | |
| 10 mM | 0.2991 mL | 1.4954 mL | 2.9909 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.
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