RyR2 stabilizer-1

RyR2 stabilizer-1 (compound 12a) is a potent RyR2 stabilizer and SERCA2a activator with EC50s of 2.7 μM for RyR2 and 383 nM for SERCA2. RyR2 stabilizer-1 inhibits Ca2+ leakage from the SR RyR2 while promoting SERCA2 to pump Ca2+ back to SR, which make RyR2 stabilizer-1 possible to prevent cardiac arrhythmias[1].

Product Specifications

CAS Number

[3012675-16-7]

UNSPSC

12352005

Target

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/ryr2-stabilizer-1.html

Solubility

10 mM in DMSO

Smiles

OC1(CCCCN(CCCCN2CC3=C(SCC2)C=CC(OC)=C3)CCCCC4(CC4)O)CC1

Molecular Formula

C28H46N2O3S

Molecular Weight

490.74

References & Citations

[1]Gyuzel Y. Mitronova, et al. 1,4-Benzothiazepines with Cyclopropanol Groups and Their Structural Analogues Exhibit Both RyR2-Stabilizing and SERCA2aStimulating Activities. Journal of Medicinal Chemistry. 2023, Article ASAP.