Description: Pazufloxacin Mesylate (T-3761), the mesylate salt of Pazufloxacin, is a fluoroquinolone-class antibiotic with a broad spectrum of antibacterial activity against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa.

Physicochemical Properties

Molecular Formula	C17H19FN2O7S
Molecular Weight	414.4044
Exact Mass	414.089
Elemental Analysis	C, 49.27; H, 4.62; F, 4.58; N, 6.76; O, 27.03; S, 7.74
CAS #	163680-77-1
Related CAS #	Pazufloxacin;127045-41-4
PubChem CID	6918232
Appearance	Solid powder
Boiling Point	531.5ºC at 760 mmHg
Melting Point	>255°C (dec.)
Flash Point	275.2ºC
Vapour Pressure	4E-12mmHg at 25°C
LogP	3.025
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	2
Heavy Atom Count	28
Complexity	695
Defined Atom Stereocenter Count	1
SMILES	O=C(C(C1=O)=CN2[C@@H](C)COC3=C(C4(N)CC4)C(F)=CC1=C23)O.CS(=O)(O)=O
InChi Key	UDHGFPATQWQARM-FJXQXJEOSA-N
InChi Code	InChI=1S/C16H15FN2O4.CH4O3S/c1-7-6-23-14-11(16(18)2-3-16)10(17)4-8-12(14)19(7)5-9(13(8)20)15(21)221-5(2,3)4/h4-5,7H,2-3,6,18H2,1H3,(H,21,22)1H3,(H,2,3,4)/t7-/m0./s1
Chemical Name	(S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid compound with methanesulfonic acid (1
Synonyms	Pazufloxacin Mesylate; Pazucross; Pasil; T-3762; T 3762; T3762
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

References

[1].Fukuoka, Y., et al., In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimicrob Agents Chemother, 1993. 37(3): p. 384-92. [2].Muratani, T., M. Inoue, and S. Mitsuhashi, In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother, 1992. 36(10): p. 2293-303.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~241.31 mM ) H2O : ≥ 100 mg/mL (~241.31 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 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: ≥ 2.5 mg/mL (6.03 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 25.0 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: ≥ 2.5 mg/mL (6.03 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (6.03 mM) Solubility in Formulation 5: 150 mg/mL (361.96 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4131 mL	12.0656 mL	24.1313 mL
	5 mM	0.4826 mL	2.4131 mL	4.8263 mL
	10 mM	0.2413 mL	1.2066 mL	2.4131 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.