1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. RyR2 stabilizer-1

RyR2 stabilizer-1 (化合物12a) 是一种有效的 RyR2 稳定剂和 SERCA2a 激活剂,对 RyR2 和 SERCA2 的 EC50 分别为 2.7 μM 和 383 nM。RyR2 stabilizer-1 抑制 Ca2+ 从 SR RyR2 渗漏,同时促进 SERCA2 将 Ca2+ 泵回 SR,这使 RyR2 stabilizer-1 有预防心律失常的可能。

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RyR2 stabilizer-1 Chemical Structure

RyR2 stabilizer-1 Chemical Structure

CAS No. : 3012675-16-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

Ryanodine receptor type 2 (RyR2) EC50: 2.7 μM (HEK-293)[1]; sarco/endoplasmic reticulum Ca2+-ATPase 2a (SERCA2a) EC50: 383 nM(mouse SR)[1]

体外研究
(In Vitro)

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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

490.74

Formula

C28H46N2O3S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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