S107 is an orally available, blood-brain barrier-permeable compound that stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. This stabilization inhibits calcium leakage from the sarcoplasmic reticulum (SR), preventing cardiac arrhythmias and raising the seizure threshold.
S107 has shown therapeutic potential in managing RBM20 cardiomyopathy by restoring elevated intracellular calcium levels to normal and improving cardiomyocyte contractile properties in isolated cardiomyocytes from Rbm20 knockout rats.
However, in vivo studies on Rbm20 knockout rats did not show significant improvement in cardiac function after S107 treatment, suggesting the need for further investigation into its efficacy and optimal treatment protocols.
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| Other Names | S107 free base |
|---|---|
| IUPAC Name | 7-methoxy-4-methyl-3, 5-dihydro-2H-1, 4-benzothiazepine |
| CAS | 927871-76-9 |
| Molecular Weight | 209.31 |
| Molecular Formula | C11H15NOS |
| SMILES | CN1CCSC2=C(C1)C=C(C=C2)OC |