Tosufloxacin tosylate hydrate, 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.

Physicochemical Properties

Molecular Formula	C26H25F3N4O7S
Molecular Weight	594.56
Exact Mass	594.14
CAS #	1400591-39-0
Related CAS #	Tosufloxacin;100490-36-6;Tosufloxacin tosylate;115964-29-9
PubChem CID	5282468
Appearance	White to off-white solid powder
LogP	5.062
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	14
Rotatable Bond Count	4
Heavy Atom Count	41
Complexity	915
Defined Atom Stereocenter Count	0
InChi Key	SSULTCPIIYRGFQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C19H15F3N4O3.C7H8O3S.H2O/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)7-25;1-6-2-4-7(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);1H2
Chemical Name	7-(3-aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid;4-methylbenzenesulfonic acid;hydrate
Synonyms	A-61827 tosylate hydrateA61827 tosylate hydrateA 61827 tosylate hydrateT-3262T 3262
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Quinolone
ln Vitro	Antibacterial activities against S. aureus, Staphylococcus epidermidis, streptococci, enterococci, Bacteroides fragilis, Clostridium difficile, and Clostridium perfringens have been demonstrated by tosufloxacin tosylate hydrate (T-3262) (0.05-3.13 μg/mL; 18 h)[2].
ln Vivo	The antibacterial activity of tosufloxacin tosylate hydrate (T-3262) (oral gavage; 0.16–13.39 mg/kg; once) against S. aureus, E. coli, and P. aeruginosa has been demonstrated in vivo[2].
Cell Assay	Cell Line: Staphylococcus epidermidis, S. aureus, Bacteroides fragilis, Clostridium difficile, and Clostridium perfringens are among the bacteria that can cause food poisoning. Concentration: 0.05-3.13 μg/mL Incubation Time: 18 hours Result: Showed MIC90s (MICs for 90% of the isolates tested) ranging from 0.05 to 1.56 μg/mL for S. aureus, Staphylococcus epidermidis, streptococci, and enterococci. Showed MIC90s of 1.56, 3.13, and 0.20 μg/mL for Bacteroides fragilis, Clostridium difficile, and Clostridium perfringens, respectively.
Animal Protocol	Animal Model: Male Slc:ICR mice infected with S. aureus[2] Dosage: 1.27-2.15 mg/kg Administration: Oral gavage; 1.27-2.15 mg/kg; once Result: demonstrated a 1.62 mg/kg (body weight) 50% effective dose (ED50) seven days post-infection. revealed a MIC of 0.0125 μg/mL.
References	[1]. Synthesis and biological properties of A-71497: a prodrug of tosufloxacin. Drugs Exp Clin Res. 1990;16(9):435-43. [2]. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827-33.
Additional Infomation	Tosufloxacin tosylate hydrate is a racemate comprising equimolar amounts of (R)- and (S)-tosufloxacin tosylate hydrate. It has a role as an antimicrobial agent, an antiinfective agent, a DNA synthesis inhibitor, a hepatotoxic agent and a topoisomerase IV inhibitor. It contains a (S)-tosufloxacin tosylate hydrate, a (R)-tosufloxacin tosylate hydrate and a tosufloxacin tosylate.

Solubility Data

Solubility (In Vitro)

DMSO : ~12.5 mg/mL (~21.02 mM) H2O : ~1 mg/mL (~1.68 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 1.25 mg/mL (2.10 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. Solubility in Formulation 3: ≥ 1.25 mg/mL (2.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.6819 mL	8.4096 mL	16.8192 mL
	5 mM	0.3364 mL	1.6819 mL	3.3638 mL
	10 mM	0.1682 mL	0.8410 mL	1.6819 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.