72956-35-5

Usage

Uses

Used in Pharmaceutical Industry:
N-Methyl Carvedilol (Carvedilol impurity) is used as a reference standard for quality control and analytical testing in the synthesis and production of Carvedilol. It helps ensure the purity, potency, and safety of the final drug product.
Additionally, it may be used in research and development for the investigation of its potential effects and interactions with Carvedilol, as well as for the development of new pharmaceutical compounds and formulations.

Upstream product

• 72956-09-3 carvedilol 
• 74-88-4 methyl iodide 
• 1836-62-0 2-(2-methoxy-phenoxy)-ethylamine 
• 51997-51-4 4-(2,3-epoxypropoxy)carbazole 

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.

Ryanodine receptor inhibitors and methods relating thereto

The present invention provides novel ryanodine receptor type 2 (RyR2) inhibitors and methods of their use in the treatment of cardiac conditions. In general, the RyR2 inhibitors of the present invention assist in the normalization of intracellular calcium homeostasis. In certain embodiments, the RyR2 inhibitors are store-overload-induced Ca2+ release (SOICR) inhibitors that minimally inhibit or do not inhibit Ca2+-induced Ca2+ release (CICR), thereby providing beneficial effects in cardiac therapy.