DRAinh-A250

DRAinh-A250 is an orally active inhibitor of mouse and human SLC26A3 (DRA). DRAinh-A250 inhibits SLC26A3-mediated anion transport, blocks colonic fluid absorption, reduces luminal fluid alkalization in the distal colonic loops of mice, and alleviates Loperamide (HY-156131)-induced constipation in wild-type and cystic fibrosis mice. DRAinh-A250 can be used in the research of constipation and cystic fibrosis-related constipation^[1][2]. In Vitro:DRAinh-A250 (compound 4ba) (0.001-1 μM) potently inhibits slc26a3-mediated chloride/iodide exchange in Fischer rat thyroid cells expressing mouse slc26a3 and halide-sensitive yellow fluorescent protein, with an IC₅₀ of 0.15 μM^[1].
DRAinh-A250 (0.02-12.5 μM) potently inhibits mouse slc26a3-mediated Cl⁻/HCO₃⁻ exchange in FRT cells, with an IC₅₀ of approximately 0.1 μM^[2].
DRAinh-A250 (0.01-3 μM) inhibits Cl⁻/SCN⁻ exchange mediated by mouse slc26a3 in FRT cells, with an IC₅₀ of approximately 0.3 μM^[2].
DRAinh-A250 (1 μM; 0-5 min for inhibition kinetics, 10 min for reversibility washout) rapidly inhibits mouse slc26a3-mediated Cl⁻/I⁻ exchange in FRT-YFP-slc26a3 cells^[2].
DRAinh-A250 (0.156-1.25 μM) potently inhibits human SLC26A3-mediated Cl⁻/I⁻ exchange in HEK cells, with an IC₅₀ of approximately 0.25 μM^[2].
DRAinh-A250 (10 μM; 24 h) shows no cytotoxicity to T84 cells after 24-hour incubation^[2]. In Vivo:DRAinh-A250 (compound 4ba) (5 mg/kg; p.o.; single dose) exhibits in vivo effects similar to those of compound 4be in a loperamide (HY-156131)-induced constipation mouse model^[1].
DRAinh-A250 (5 mg/kg; p.o.; single dose) partially reverses loperamide-induced constipation in wild-type mice and significantly alleviates loperamide-induced constipation in cystic fibrosis mice^[2].