RyR1 inhibitor compound 1 is a potent, RyR1-selective inhibitor, inhibits the RyR1 channel with IC50 of 12 nM in HEK293 cell-based assay.
RyR1 inhibitor compound 1 sodium salt exhibited good solubility in normal saline (0.9% NaCl) as well as pure water and glucose solution, with extremely high potency which is comparable to dantrolene in in vitro study.
RyR1 inhibitor compound 1 reduces resting intracellular Ca2+, inhibits halothane- and isoflurane-induced Ca2+ release, suppresses caffeine-induced contracture in skeletal muscle, reduces sarcolemmal cation influx, and prevents or reverses the fulminant MH crisis induced by isoflurane anesthesia.
RyR1 inhibitor compound 1 rescues animals from heat stroke caused by environmental heat stress.
