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S107

Catalog No. T3438 CAS 927871-76-9

S107 is a RyR-selective 1, 4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.

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S107, CAS 927871-76-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 267.00
50 mg	In stock	$ 447.00
100 mg	In stock	$ 637.00
1 mL * 10 mM (in DMSO)	In stock	$ 107.00

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Purity: 99.63%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	S107 is a RyR-selective 1, 4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.
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 has no effect on cardiac ion channels including the voltage-gated Na+, K+, and Ca2+ channels at concentrations up to 10 μM, and S107 had no effect on normal Ca2+ signaling in cells[1]. S107 is a promising candidate drug for treating catecholaminergic polymorphic ventricular tachycardia (CPVT). 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 is thought to improve skeletal muscle function by stabilizing the RyR1-FKBP12 complex. 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 effectively inhibits seizures and arrhythmias in mutant mice without blocking the channel or changing normal calcium (Ca2+) signaling; it specifically prevents leakage in the channel[1].

Molecular Weight	209.31
Formula	C11H15NOS
CAS No.	927871-76-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 38 mg/mL

References and Literature

1. Lehnart SE, et al. Leaky Ca 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):e20164795. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max Anti-Diabetic Compound Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Anti-Alzheimer's Disease Compound Library

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Keywords

S107 927871-76-9 Others S 107 S-107 inhibitor inhibit

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