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Usage

Uses

Used in Pharmaceutical Industry:
2,3,4,5-Tetrahydro-7-methoxy-4-methyl-1,4-benzothiazepine is used as a therapeutic agent for muscle-related conditions. Its application is based on its capacity to prevent the depletion of Calstabin-1 from the RyR1 complex, which in turn slows muscle fatigue and reduces muscle damage in exercised mice.
Used in Muscular Dystrophy Treatment:
In a murine model of Duchenne muscular dystrophy, 2,3,4,5-Tetrahydro-7-methoxy-4-methyl-1,4-benzothiazepine, also known as S 107, demonstrates significant benefits. It reduces biochemical and histological evidence of muscle damage associated with muscular dystrophy, improves muscle function, and enhances exercise performance, offering a promising avenue for the treatment of this debilitating condition.

Upstream product

• 13735-11-0 6-methoxy-2,3-dihydro-4H-thiochromen-4-one 
• 145903-32-8 7-methoxy-3,4-dihydrobenzo[f][1,4]thiazepin-5(2H)-one 
• 145903-31-7 7-methoxy-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine 
• 50-00-0 formaldehyd 
• 696-63-9 4-Methoxybenzenethiol 
• 13739-36-1 β-(4-methoxyphenylmercapto)propionic acid 

Relevant academic research and scientific papers

STORE OVERLOAD-INDUCED CALCIUM RELEASE INHIBITORS AND METHODS FOR PRODUCING AND USING THE SAME

The present invention provides compounds having store overload-induced Ca2+ release (SOICR) inhibitory activity and methods for producing and using the same. In particular, compounds of the invention is of the formula: R1-X1-L-X2-R2, wherein R1, X1, L, X2, and R2 are those defined herein.

Novel carvedilol analogues that suppress store-overload-induced Ca 2+ release

Carvedilol is a uniquely effective drug for the treatment of cardiac arrhythmias in patients with heart failure. This activity is in part because of its ability to inhibit store-overload-induced calcium release (SOICR) through the RyR2 channel. We describe the synthesis, characterization, and bioassay of ca. 100 compounds based on the carvedilol motif to identify features that correlate with and optimize SOICR inhibition. A single-cell bioassay was employed on the basis of the RyR2-R4496C mutant HEK-293 cell line in which calcium release from the endoplasmic reticulum through the defective channel was measured. IC50 values for SOICR inhibition were thus obtained. The compounds investigated contained modifications to the three principal subunits of carvedilol, including the carbazole and catechol moieties, as well as the linker chain containing the β-amino alcohol functionality. The SAR results indicate that significant alterations are tolerated in each of the three subunits.