Drug intelligence / Profile preview

405-1

Development stage
Preclinical
Lead developer
Columbia University
Modality
Small Molecules
01

Overview

405-1 is a metabolite-inspired synthetic derivative of ginger-based compounds, such as 6-shogaol, currently under investigation for the treatment of vascular hypertensive disorders, specifically pulmonary hypertension. Developed through research at Columbia University and North Carolina Agricultural and Technical State University, 405-1 functions as an inhibitor of phospholipase C (PLC). By inhibiting PLC, the compound attenuates the increase of intracellular calcium in pulmonary artery smooth muscle cells (PASMC) typically stimulated by vasoconstrictors like endothelin 1 (ET1). This mechanism leads to the relaxation of pre-contracted pulmonary arteries, suggesting potential therapeutic utility in managing the vascular hyperreactivity and hypertrophy associated with pulmonary hypertension.

02

Targets

PLC (Phospholipase C family)

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