vericiguat

China [CN]

I. Basic Information

Item Details

English Name Vericiguat

Chinese Name 维立西呱 (Weiliciguat)

Chemical Name Methyl {4,6-diamino-2-[5-fluoro-1-[(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate

CAS Number 1552050-06-5

Molecular Formula C₁₉H₁₆F₂N₈O₂

Molecular Weight 426.39

Target Soluble Guanylate Cyclase (sGC)

Developer Jointly developed by Merck and Bayer

Marketed January 2021 (US FDA); May 2022 (China NMPA)

Trade Name Verquvo

Dosage Form 2.5mg, 5mg, 10mg film-coated tablets

II. Physicochemical Properties

Parameter Data

Appearance White to off-white crystalline powder

Solubility Slightly soluble in water, readily soluble in dimethyl sulfoxide, soluble in methanol

Dissociation Constant (pKa) 7.4 (predicted value)

Stability Stable for 24 months at 25°C/60% RH, avoid high temperature, light and moisture

Storage Conditions Store at 20-25°C in a sealed container, short-term excursions between 15-30°C are permitted

III. Mechanism of Action

Vericiguat is a direct sGC stimulator, with the following mechanism of action:

Directly activates sGC (NO-independent) and enhances the sensitivity of sGC to NO.

Promotes cGMP synthesis, mediating smooth muscle relaxation and vasodilation, reducing cardiac preload and afterload, and improving cardiac pumping function.

Inhibits myocardial remodeling and delays the progression of heart failure.