Description: Trovafloxacin mesylate (CP-99219) is a broad-spectrum quinolone antibiotic that inhibits DNA supercoiling in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It has potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a highly potent, specific and orally bioavailable pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
References:
[1]. Giustarini G, et al. The hepatotoxic fluoroquinolone trovafloxacin disturbs TNF- and LPS-induced p65 nuclear translocation in vivo and in vitro. Toxicol Appl Pharmacol. 2020 Mar 15;391:114915.
[2]. Poon IK, et al. Unexpected link between an antibiotic, pannexin channels and apoptosis. Nature. 2014 Mar 20;507(7492):329-34.
[3]. Gootz TD, et al. Activity of the new fluoroquinolone trovafloxacin (CP-99,219) against DNA gyrase and topoisomerase IV mutants of Streptococcus pneumoniae selected in vitro. Antimicrob Agents Chemother. 1996 Dec;40(12):2691-7.
Related CAS #: 147059-75-4 (mesylate) 147059-72-1 (free base)