| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Amifloxacin targets bacterial DNA gyrase (topoisomerase II) and inhibits DNA and RNA synthesis in bacteria, leading to bacterial cell death; this mechanism is characteristic of fluoroquinolone antibiotics.
|
|---|---|
| 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.
In vitro studies demonstrate that Amifloxacin is active against Pseudomonas aeruginosa isolates and shows moderate activity against Staphylococcus aureus, with minimum inhibitory concentrations (MICs) of ≤2 μg/mL; it also exhibits broad-spectrum activity against both Gram-positive and Gram-negative bacteria. |
| 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].
In vivo, Amifloxacin has been used to treat various bacterial infections including pneumonia, bronchitis, pharyngitis, tonsillitis, pyelonephritis, urinary tract infections, gonococcal urethritis, cholecystitis, and cholangitis, showing efficacy comparable to norfloxacin. |
| Enzyme Assay |
The in vitro antimicrobial susceptibility assay involves incubating Amifloxacin with bacterial isolates in broth medium, determining the minimum inhibitory concentration (MIC) by serial dilution methods according to CLSI guidelines, and measuring optical density at 600 nm to assess bacterial growth inhibition.
|
| Cell Assay |
In vitro cell culture studies are not typically performed for antibiotics; instead, bacterial culture assays are used to evaluate antibacterial activity, with time-kill curves generated to assess bactericidal kinetics and combination studies performed to evaluate synergy with other antibiotics.
|
| Animal Protocol |
In vivo animal models for evaluating Amifloxacin include murine models of bacterial infection (e.g., sepsis, pneumonia), where the compound is administered via oral or parenteral routes, with bacterial load assessed in blood or target organs, and survival outcomes monitored over 7-14 days.
|
| ADME/Pharmacokinetics |
Amifloxacin has the molecular formula C16H19FN4O3 and is a synthetic fluoroquinolone; it is typically stored as a solid powder at room temperature, with purity ≥98%, and is soluble in DMSO and aqueous solutions; it was first introduced in Japan in 1986.
|
| Toxicity/Toxicokinetics |
Toxicological data for Amifloxacin include typical fluoroquinolone side effects such as gastrointestinal disturbances, central nervous system effects, and potential cartilage toxicity in juvenile animals; it is contraindicated in children and pregnant women due to concerns about arthropathy.
|
| 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 belongs to the quinoline class of drugs.
Amifloxacin (WIN 49375) is a fluoroquinolone antibiotic that has been used clinically for the treatment of bacterial infections; it shows no cross-resistance with other antibiotic classes, though resistance can develop through mutations in DNA gyrase or efflux pump overexpression; its clinical use has been largely superseded by newer fluoroquinolones. |
| Molecular Formula |
C16H19FN4O3
|
|---|---|
| Molecular Weight |
334.3455
|
| Exact Mass |
334.144
|
| CAS # |
86393-37-5
|
| Related CAS # |
88036-80-0 (mesylate);86393-37-5;
|
| PubChem CID |
55492
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.44g/cm3
|
| Boiling Point |
532.5ºC at 760mmHg
|
| Melting Point |
300 °C
|
| Flash Point |
275.8ºC
|
| Index of Refraction |
1.662
|
| LogP |
0.839
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
547
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C(=O)C2C(=CC(N3CCN(C)CC3)=C(C=2)F)N(NC)C=1)O
|
| InChi Key |
RUXPNBWPIRDVTH-UHFFFAOYSA-N
|
| 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)
|
| Chemical Name |
6-fluoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~50 mg/mL (~149.54 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
