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S107 hydrochloride 

Cat. No.: HY-15292A Purity: 99.77%
Handling Instructions

S107 hydrochloride 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.

For research use only. We do not sell to patients.

S107 hydrochloride Chemical Structure

S107 hydrochloride Chemical Structure

CAS No. : 1357476-46-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 770 In-stock
Estimated Time of Arrival: December 31
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Other Forms of S107 hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

S107 hydrochloride 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, 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].

Solvent & Solubility
In Vitro: 

H2O : ≥ 132 mg/mL (537.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0688 mL 20.3442 mL 40.6884 mL
5 mM 0.8138 mL 4.0688 mL 8.1377 mL
10 mM 0.4069 mL 2.0344 mL 4.0688 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]

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].

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

References
Molecular Weight

245.77

Formula

C₁₁H₁₆ClNOS

CAS No.

1357476-46-0

SMILES

COC1=CC=C2SCCN(CC2=C1)C.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
S107 hydrochloride
Cat. No.:
HY-15292A
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S107 hydrochloride

Cat. No.: HY-15292A