| Bioactivity | 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]. |
| Target | Ryanodine receptor type 2 (RyR2) EC50: 2.7 μM (HEK-293);sarco/endoplasmic reticulum Ca2+-ATPase 2a (SERCA2a) EC50: 383 nM(mouse SR) |
| Invitro | RyR2 stabilizer-1 (0~100 μM) 剂量依赖性地显著增加了 [Ca2+]ER, 在 25 μM 以上的浓度中 RyR2 stabilizer-1 显示出最显著的效果[1]。RyR2 stabilizer-1 对小鼠 SR、HL-1 和 HEK ER 中 SERCA2a 的EC50s分别为 383 nM， 9.2 μM 和 16 nM[1]。RyR2 stabilizer-1 (10 μM 孵育 2 小时) 在咖啡因诱导的钙离子释放试验中提升了 HL-1 SERCA2a 活性[1]。RyR2 stabilizer-1 (0-50 μM，HL-1，24 小时) 在 CytoTox-Glo 细胞毒性试验中未显示出明显的细胞死亡[1]。RyR2 stabilizer-1 (100 μM，5 分钟) 导致 NADH 荧光的强烈下降，反映出小鼠心室 SR 微粒体中 SERCA2a 活性的升高，它也导致了 ATP 酶活性的升高 [1]。 0 --> RyR2 stabilizer-1 相关抗体: |
| Name | RyR2 stabilizer-1 |
| Formula | C28H46N2O3S |
| Molar Mass | 490.74 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |