JTV-519 fumarate

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs); displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle; 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). Heart Arrhythmia Phase 2 Discontinued

References 1. Darcy YL, et al. Mol Pharmacol. 2016 Aug;90(2):106-15. 2. Inagaki K, et al. Circulation. 2000 Feb 22;101(7):797-804. 3. Ito K, et al. Br J Pharmacol. 2000 Jun;130(4):767-76. 4. Nakaya H, et al. Br J Pharmacol. 2000 Dec;131(7):1363-72. View Related Products by Target Calcium Channel Heart Arrhythmia