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Pazufloxacin Mesylate

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Chemical Structure| 163680-77-1 同义名 : 帕珠沙星甲磺酸盐 ;T-3762;Pazufloxacin methanesulfonate;Pazufloxacin (mesylate);Pazucross;Pazufloxacin mesilate
CAS号 : 163680-77-1
货号 : A395221
分子式 : C17H19FN2O7S
纯度 : 98%
分子量 : 414.405
MDL号 : MFCD00913262
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(253.38 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(241.31 mM)
动物实验配方：
生物活性
描述 Pazufloxacin Mesylate (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. Its MICs for 90% of the strains tested were 0.20 to 100 micrograms/ml against gram-positive bacteria, including members of the genera Staphylococcus, Streptococcus, and Enterococcus; 0.025 to 3.13 micrograms/ml against gram-negative bacteria, including members of the family Enterobacteriaceae and the genus Haemophilus; 0.05 to 50 micrograms/ml against glucose nonfermenters, including members of the genera Pseudomonas, Xanthomonas, Acinetobacter, Alcaligenes, and Moraxella; 0.025 micrograms/ml against Legionella spp.; and 6.25 to 25 micrograms/ml against anaerobes, including Bacteroides fragilis, Clostridium difficile, and Peptostreptococcus spp[3]. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively[4]. All regimens of pazufloxacin administration were well tolerated. Pazufloxacin exhibits lack of dose proportionality over the dose range of 300 - 1,000 mg[5]. Pazufloxacin methanesulphonate at the dose of 300 mg and 500 mg have similar efficacy in treating acute bacterial infections. The dosage regimen of 300 mg Q12h intravenous infusion is recommended[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.07mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL
参考文献

[1]Khan AM, Rampal S. Effects of repeated oral administration of pazufloxacin mesylate and meloxicam on the antioxidant status in rabbits. J Am Assoc Lab Anim Sci. 2014 Jul;53(4):399-403.

[2]Muratani T, Inoue M, et al. In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother. 1992 Oct;36(10):2293-303.

[3]Fukuoka Y, Ikeda Y, Yamashiro Y, Takahata M, Todo Y, Narita H. In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimicrob Agents Chemother. 1993;37(3):384–392

[4]Muratani T, Inoue M, Mitsuhashi S. In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother. 1992;36(10):2293–2303

[5]Lee J, Seong SJ, Lim MS, et al. Single-dose pharmacokinetics and dose proportionality of intravenous pazufloxacin mesilate in healthy Korean volunteers. Expert Opin Drug Metab Toxicol. 2012;8(8):921–928

[6]Wang XG, Miao J, Liang DR, Yu Q, Liang MZ, Zhang SH. Sichuan Da Xue Xue Bao Yi Xue Ban. 2009;40(4):689–693