Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
Antagonist activity at TRPV1 in C57/BL6 mouse cerebellar granule cells assessed as inhibition of KCl-induced voltage dependent calcium entry at 10 uM by fura-2-based assay
Antagonist activity at TRPM8 in C57/BL6 mouse cerebellar granule cells assessed as inhibition of KCl-induced voltage dependent calcium entry at 10 uM by fura-2-based assay
Antagonist activity at TRPV1 (unknown origin) expressed in HEK cells assessed as inhibition of capsaicin-induced calcium increase at 10 uM by fura-2-based assay
Antagonist activity at TRPM8 (unknown origin) expressed in HEK cells assessed as inhibition of menthol -mediated calcium increase at 10 uM by fura-2-based assay
Drug metabolism in CD1 mouse liver microsomes assessed as (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(3-(1-(4-(4-(isopropoxycarbonyl)-5-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-1H-1,2,3-triazol-4-yl)benzoyloxy)tetrahydro-2H-pyran-2-carboxylic acid metabolite formation at 50 uM after 60 mins by mass spectroscopic analysis
Drug metabolism in CD1 mouse liver microsomes assessed as 1-(4-(4-(3-Carboxyphenyl)-1H-1,2,3-triazol-1-yl)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic Acid metabolite formation at 50 uM after 60 mins by mass spectroscopic analysis