TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel ( ZAC ) antagonist. TTFB inhibits Zn 2+ - and H + -induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
In Vitro, TTFB (0.1-100 μM; 30 seconds) potently inhibits Zn2+-evoked, H+-evoked, and spontaneous ZAC activity in Xenopus oocytes with IC50 values of 3.0 μM, 8.5 μM, and 4.7 μM, respectively, and mediates complete inhibition of Zn2+-induced responses[1]. TTFB (10 μM) mediates ZAC inhibition that is voltage-independent, as it inhibits H+-evoked currents similarly at -60 mV and +60 mV[1].
References:
[1]. Madjroh N, et al. Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC). Biochem Pharmacol. 2021;193:114782.
In Vitro, TTFB (0.1-100 μM; 30 seconds) potently inhibits Zn2+-evoked, H+-evoked, and spontaneous ZAC activity in Xenopus oocytes with IC50 values of 3.0 μM, 8.5 μM, and 4.7 μM, respectively, and mediates complete inhibition of Zn2+-induced responses[1]. TTFB (10 μM) mediates ZAC inhibition that is voltage-independent, as it inhibits H+-evoked currents similarly at -60 mV and +60 mV[1].
References:
[1]. Madjroh N, et al. Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC). Biochem Pharmacol. 2021;193:114782.