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Description

A cell-permeable uricosuric agent that, in addition to its known efficacy in gout treatment, acts as a reversible CaCC blocker and is reported to be more potent than NFA (Cat. No. 481987) and NPPB (Cat. No. 484100) in suppressing 500 nM Ionomycin- (Cat. Nos. 407950, 407952, and 407953) induced I- influx in TMEM16A-expressing HEK293 cells (IC50 = 9.97, 140, and 150 µ,M, respectively) as well as in blocking voltage-gated Cl- current in TMEM16B-expressing HEK293 cells, while exhibiting much reduced potency against ENaC (alpha, beta, and gamma) or CFTR. Shown to significantly reduce mucin secretion from NHBE (normal human bronchial epithelial) and suppress human ASM (airway smooth muscle) contraction upon muscarinic receptor stimulation., A cell-permeable uricosuric agent that, in addition to its known efficacy in gout treatment, acts as a reversible CaCC blocker and is reported to be more potent than NFA (Cat. No. 481987) and NPPB (Cat. No. 484100) in suppressing 500 nM Ionomycin- (Cat. Nos. 407950, 407952, and 407953) induced I- influx in TMEM16A-expressing HEK293 cells (IC50 = 9.97, 140, and 150 µ,M, respectively) as well as in blocking voltage-gated Cl- current in TMEM16B-expressing HEK293 (64% inhibition with 10 µ,M BBR vs. 47% inhibition with 300 µ,M NFA, by whole cell patch clamp), while exhibiting much reduced potency against voltage-gated current via ENaC (alpha, beta, and gamma) or CFTR (by 25% and 17% with 10 µ,M BBR, respectively, using HEK293 ENaC or CFTR transfectants). Shown to significantly reduce 100 µ,M ATP-induced CaCC current (IAC current = 1.137 vs. 3.099 µ,A/cm2 with or without 10 µ,M BBR) and mucin secretion from NHBE (normal human bronchial epithelial) as well as suppress human ASM (airway smooth muscle) contraction upon muscarinic receptor stimulation.