JTV-519 (hemifumarate)

JTV-519 (hemifumarate)

• CAS Number: 1435938-25-2
• UNSPSC Description: JTV-519 hemifumarate (K201 hemifumarate) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties[1][2].
• Target Antigen: Calcium Channel
• Type: Reference compound
• Related Pathways: Membrane Transporter/Ion Channel;Neuronal Signaling
• Applications: Neuroscience-Neuromodulation
• Field of Research: Cardiovascular Disease
• Assay Protocol: https://www.medchemexpress.com/jtv-519-hemifumarate.html
• Solubility: DMSO : 100 mg/mL (ultrasonic)
• Smiles: O=C(N1CCSC2=CC=C(OC)C=C2C1)CCN3CCC(CC4=CC=CC=C4)CC3.O=C(O)/C=C/C(O)=O.[1/2]
• Molecular Weight: 482.64
• References & Citations: [1]Darcy YL, et al. K201 (JTV519) is a Ca²⁺-Dependent Blocker of SERCA and a Partial Agonist of Ryanodine Receptors in Striated Muscle. Mol Pharmacol. 2016 Aug;90(2):106-15.|[2]Kaneko N, et al. Inhibition of annexin V-dependent Ca2+ movement in large unilamellar vesicles by K201, a new 1,4-benzothiazepine derivative. Biochim Biophys Acta. 1997 Nov 13;1330(1):1-7.|[3]Yang J, et al. Toll-like receptor 4-induced ryanodine receptor 2 oxidation and sarcoplasmic reticulum Ca²⁺ leakage promote cardiac contractile dysfunction in sepsis. J Biol Chem. 2018 Jan 19;293(3):794-807.
• Shipping Conditions: Room Temperature
• Clinical Information: Phase 2