tcsc1169 Cinaciguat

Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.



In Vitro: Cinaciguat (10 μM) significantly enhances intracellular cGMP generation. Cinaciguat does not dose-dependent effects on cell contraction and calcium transients^[2].

In Vivo: Cinaciguat (10 mg/kg/day, p.o.) treatment in diabetic rats does not influence blood glucose levels, but leads to attenuated water intake. Cinaciguat treatment alleviates diabetes mellitus related oxidative stress, protects against DM related alteration of the NO-sGC-cGMP-PKG signalling, and alleviates DM related myocardium hypertrophy and apoptosis^[1]. Cinaciguat (1-10-100 nM) induces concentration-dependent relaxations in strips from both WT and apo-sGC mice, but does not have any effect on phasic activity induced by PGF_2α in WT or apo-sGC strips^[3].