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Tosufloxacin tosylate (A61827)

Alias: T-3262 T3262 T 3262 Tosufloxacin tosylate
Cat No.:V12793 Purity: ≥98%
Tosufloxacin tosylate, formerly known as T-3262 andA-61827, is a potent fluoroquinolone antibiotic used to treat susceptible infections.
Tosufloxacin tosylate (A61827)
Tosufloxacin tosylate (A61827) Chemical Structure CAS No.: 115964-29-9
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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25mg
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1g
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Other Forms of Tosufloxacin tosylate (A61827):

  • Tosufloxacin tosylate hydrate (T3262, A61827)
  • Tosufloxacin (T3262, A61827)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Tosufloxacin tosylate, formerly known as T-3262 and A-61827, is a potent fluoroquinolone antibiotic used to treat susceptible infections. It has a controversial safety profile in relation to other fluoroquinolones. It is associated with severe thrombocytopenia and nephritis, and hepatotoxicity. It is sold in Japan under the brand name Ozex.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Tosifloxacin tosylate hydrate (T-3262) (0.05-3.13 μg/mL; 18 h) possesses antibacterial action that is effective against Streptococcus, Enterococcus, Bacteroides fragilis, Clostridium difficile, and Clostridium perfringens [2].
ln Vivo
Sufloxacin tosylate hydrate (T-3262) treatment (oral gavage; 0.16–13.39 mg/kg; once) showed antibacterial efficacy against Pseudomonas aeruginosa, Escherichia coli, and Staphylococcus aureus in vivo [2].
Cell Assay
Cell Viability Assay[2]
Cell Types: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus, Enterococcus, Bacteroides fragilis, Clostridium difficile and Clostridium perfringens
Tested Concentrations: 0.05-3.13 μg/mL
Incubation Duration: 18 Hourly
Experimental Results: Displays MIC90s (MIC 90) for Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus, and Enterococcus, ranging from 0.05 to 1.56 μg/mL. MIC90 values for Bacteroides fragilis, Clostridium difficile, and Clostridium perfringens were 1.56, 3.13 and 0.20 μg/mL respectively.
Animal Protocol
Animal/Disease Models: Male Slc:ICR mice infected with Staphylococcus aureus [2]
Doses: 1.27-2.15 mg/kg
Route of Administration: po (oral gavage); 1.27-2.15 mg/kg; primary
Experimental Results:7 days after infection demonstrated 50 The % effective dose (ED50) is 1.62 mg/kg (body weight). The displayed MIC value is 0.0125 μg/mL.

Animal/Disease Models: Male Slc:ICR mice infected with E. coli [2]
Doses: 0.16-0.30 mg/kg
Route of Administration: po (oral gavage); 0.16-0.30 mg/kg; Primary
Experimental Results:50% effective 7 days after infection The dose (ED50) is 0.22 mg/kg (body weight). The displayed MIC value is 0.0125 μg/mL.

Animal/Disease Models: Male Slc:ICR mice infected with Pseudomonas aeruginosa [2]
Doses: 7.66-13.39 mg/kg
Route of Administration: po (oral gavage); 7.66-13.39 mg/kg; Primary
Experimental Results:Displayed 7 days after infection The 50% effective dose (ED50) is 10.13 mg/kg (body weight). The displayed MIC value is 0.78 μg/mL.
References
[1]. Chu DT, et al. Synthesis and biological properties of A-71497: a prodrug of tosufloxacin. Drugs Exp Clin Res. 1990;16(9):435-43.
[2]. Fujimaki K, et al. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827-33.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H23F3N4O6S
Molecular Weight
576.54422
Exact Mass
404.11
Elemental Analysis
C, 54.16; H, 4.02; F, 9.89; N, 9.72; O, 16.65; S, 5.56
CAS #
115964-29-9
Related CAS #
Tosufloxacin tosylate hydrate;1400591-39-0;Tosufloxacin;100490-36-6
Appearance
Solid powder
SMILES
O=C(C1=CN(C2=CC=C(F)C=C2F)C3=NC(N4CC(N)CC4)=C(F)C=C3C1=O)O.OS(=O)(C5=CC=C(C)C=C5)=O
InChi Key
CSSQVOKOWWIUCX-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H15F3N4O3.C7H8O3S/c20-9-1-2-15(13(21)5-9)26-8-12(19(28)29)16(27)11-6-14(22)18(24-17(11)26)25-4-3-10(23)7-251-6-2-4-7(5-3-6)11(8,9)10/h1-2,5-6,8,10H,3-4,7,23H2,(H,28,29)2-5H,1H3,(H,8,9,10)
Chemical Name
7-(3-aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid tosylate
Synonyms
T-3262 T3262 T 3262 Tosufloxacin tosylate
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 Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7345 mL 8.6724 mL 17.3449 mL
5 mM 0.3469 mL 1.7345 mL 3.4690 mL
10 mM 0.1734 mL 0.8672 mL 1.7345 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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