Anti-absorptive activity in loperamide-induced CD-1 mouse model of constipation assessed as improvement in stool weight at 5 mg/kg, po administered via gavage for 1 hr prior to loperamide challenge and measured after 3 hrs
Inhibition of mouse slc26a3 expressed in FRT cells co-expressing EYFP-H148Q/I152L/F46L assessed as reduction in protein-mediated chloride/iodide exchange preincubated for 10 mins followed by NaI-substituted PBS addition and measured by YFP-based fluorescence assay
Inhibition of mouse slc26a3 expressed in FRT cells co-expressing EYFP-H148Q/I152L/F46L assessed as reduction in protein-mediated chloride/bicarbonate exchange by measuring decrease in cytoplasmic alkalinization by BCECF probe-based fluorescence assay
Inhibition of mouse slc26a4 expressed in FRT cells co-expressing EYFP-H148Q/I152L/F46L assessed as reduction in protein-mediated chloride/iodide exchange at 10 uM preincubated for 10 mins followed by NaI-substituted PBS addition and measured by YFP-based fluorescence assay
Inhibition of mouse slc26a6 expressed in FRT cells co-expressing EYFP-H148Q/I152L/F46L assessed as reduction in protein-mediated chloride/iodide exchange at 10 uM preincubated for 10 mins followed by NaI-substituted PBS addition and measured by YFP-based fluorescence assay
Inhibition of human slc26a9 expressed in FRT cells co-expressing EYFP-H148Q/I152L/F46L assessed as reduction in protein-mediated chloride/iodide exchange at 10 uM preincubated for 10 mins followed by NaI-substituted PBS addition and measured by YFP-based fluorescence assay
Anti-absorptive activity in loperamide-induced CD-1 mouse model of constipation assessed as improvement in fecal pellet number at 5 mg/kg, po administered via gavage for 1 hr prior to loperamide challenge and measured after 3 hrs
Anti-absorptive activity in loperamide-induced CD-1 mouse model of constipation assessed as improvement in stool water content at 5 mg/kg, po administered via gavage for 1 hr prior to loperamide challenge and measured after 3 hrs
In vivo inhibition of slc26a3 in loperamide-induced constipation model of female CD-1 mouse at 5 mg/kg, po assessed as reduction in stool water content