Drug intelligence / Profile preview

HC-030031

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

HC-030031 is a small molecule research compound that acts as a potent and selective antagonist of the Transient Receptor Potential Ankyrin 1 (TRPA1) receptor. Chemically, it is a substituted theophylline derivative, specifically 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide. Developed by Merck Research Laboratories, the compound has been widely used as a pharmacological tool to study TRPA1 function in preclinical models of inflammatory and neuropathic pain, where it has demonstrated efficacy in reducing mechanical hypersensitivity. It exhibits high selectivity for TRPA1 over other TRP channels (TRPV1, TRPV3, TRPV4) and other ion channels like hERG and NaV1.2. Recent research has also utilized HC-030031 to investigate the CaMKII-TRPA1 axis in small cell lung cancer (SCLC) metabolism, where TRPA1 activation is linked to ATP release and autocrine signaling. Despite its extensive use in research, there is no evidence that HC-030031 has entered clinical development for any therapeutic indication.

Other names
2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide
02

Targets

TRPA1 (Transient receptor potential cation channel subfamily A member 1)

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