DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
DFBTA shows very weak cytotoxicity and cardiotoxicity (HEK293 proliferation IC50 > 30 μM, hERG IC50 > 30 μM)[1]
DFBTA (C57BL/6 mice; 40-80 mg/kg, IG; 40 mg/kg, IV; once) shows weak acute toxicity, with mouse minimum lethal dosage (MLD) > 1000 mg/kg[1].
DFBTA (C57BL/6 mice, 1000 mg/kg, Orally, once) shows excellent pharmacokinetics properties with oral bioavailability > 75% and little brain penetration (<1.5% brain/plasma)[1].