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S107

MCE China：S107

Brand：MedChemExpress (MCE)

Cat. No.HY-15292

CAS：927871-76-9

Purity：99.77%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.

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[1]. 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%[2]. 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[3].

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[1].

Animal Administration：Mice: To test for protection against seizures using S107, osmotic pumps are implanted, and mice are pretreated with S107 5 mg/kg/h for 1 week prior to seizure susceptibility testing. Phase 4 seizures associated with death could be avoided through intubation and artificial breathing, indicating diaphragm failure during sustained seizures as a potential cause of death. Mice are directly observed and videorecorded for later review and latency classification during a 60-minute observation period[1].

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References：

[1]. Lehnart SE, et al. Leaky Ca²⁺ release channel/ryanodine receptor 2 causes seizures and sudden cardiac death in mice. J Clin Invest. 2008 Jun;118(6):2230-45.  [Content Brief]

[2]. Sasaki K, et al. Patient-Specific Human Induced Pluripotent Stem Cell Model Assessed with Electrical Pacing Validates S107 as a Potential Therapeutic Agent for Catecholaminergic Polymorphic Ventricular Tachycardia. PLoS One. 2016 Oct 20;11(10):e0164795.  [Content Brief]

[3]. Mei Y, et al. Stabilization of the skeletal muscle ryanodine receptor ion channel-FKBP12 complex by the 1,4-benzothiazepine derivative S107. PLoS One. 2013;8(1):e54208.  [Content Brief]