Pefloxacin-d₅  (Synonyms: 培氟沙星-d₅; Pefloxacinium-d₅)

Pefloxacin-d₅ is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC₅₀ of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies^{[1][2][3][4][5][6][7][8][9]}.

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^[75].

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

338.39

C₁₇H₁₅D₅FN₃O₃

1228182-51-1

70458-92-3

固体

White to off-white

培氟沙星-d₅

Room temperature in continental US; may vary elsewhere.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.  [Content Brief]