Pazufloxacin-d₄  (Synonyms: T3761-d₄)

Pazufloxacin-d₄ is deuterium labeled Pazufloxacin (HY-B0724B). Pazufloxacin is an orally active fluoroquinolone antimicrobial agent. Pazufloxacin inhibits DNA gyrase with IC₅₀ values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin exhibits broad-spectrum antimicrobial activity, with MIC₉₀ values ranging from 0.025 to 100 μg/mL against Gram-positive and Gram-negative bacteria, non-fermenting bacteria, Legionella spp., and anaerobic bacteria. Pazufloxacin is indicated for research on systemic infections, lung infections, urinary tract infections, and Legionella pneumonia^{[1][2][3][4][5][6]}.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

322.32

C₁₆H₁₁D₄FN₂O₄

1346602-96-7

127045-41-4

O=C1C2=CC(F)=C(C3(C([2H])([2H])C3([2H])[2H])N)C4=C2N(C=C1C(O)=O)[C@@H](C)CO4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. Takei M, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.  [Content Brief]

  [5]. Sousa J, et al. First liquid chromatography method for the simultaneous determination of levofloxacin, Pazufloxacin hydrochloride, gatifloxacin, moxifloxacin and trovafloxacin in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Jul 1;930:104-11.  [Content Brief]

  [6]. Morinaga Y, et al. In vivo efficacy of sivelestat in combination with Pazufloxacin hydrochloride against Legionella pneumonia. Exp Lung Res. 2010 Oct;36(8):484-90.  [Content Brief]