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S107

CAS No. : 927871⁻⁷6-9

MCE 国际站：S107

产品活性：S107 是一种口服可用的，血脑屏障可渗透的化合物，通过增强 calstabin2 与突变 Ryr2-R2474S 通道的结合来稳定 RyR2 通道。S107 抑制肌浆网 (SR) 的 Ca²⁺ 渗漏，预防心律失常，提高癫痫发作阈值。

研究领域：Others

作用靶点：Others

In Vitro: S107 is a small compound that enhances calstabin2 binding to RyR2 at low nanomolar concentrations and failed to interact with over 400 receptors, enzymes, and ion channels in screens using up to 10 µM of the compound.
S107 exerts an antiarrhythmic effect on CPVT-hiPSC-CMs. Pre-incubation with 10 µM S107, which stabilizes the closed state of the ryanodine receptor 2, significantly decreases the percentage of CPVT-hiPSC-CMs presenting DADs to 25%.
S107 increases FKBP12 binding to RyR1 in SR vesicles in the presence of reduced glutathione and the NO-donor NOC12, with no effect in the presence of oxidized glutathione. S107 can reverse the harmful effects of redox active species on SR Ca²⁺ release in skeletal muscle by binding to RyR1 low affinity sites.

In Vivo: S107, which prevents a leak in the channel but does not block the channel or alter normal Ca²⁺ signaling, is able to inhibit both seizures and arrhythymias in the mutant mice.

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