JTV-519 hemifumarate (K201) is a Ca2+-dependent blocker of SERCA and a ryanodine receptor 2 (RyR2) inhibitor.
JTV-519 displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle.
JTV-519 may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively).
