Bioactivity | Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure. | ||||||||||||
Invitro | 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 PGF2α in WT or apo-sGC strips[3]. | ||||||||||||
Name | Cinaciguat | ||||||||||||
CAS | 329773-35-5 | ||||||||||||
Formula | C36H39NO5 | ||||||||||||
Molar Mass | 565.70 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Mátyás C, et al. The soluble guanylate cyclase activator cinaciguat prevents cardiac dysfunction in a rat model of type-1 diabetes mellitus. Cardiovasc Diabetol. 2015 Oct 31;14:145. [2]. Reinke Y, et al. The soluble guanylate cyclase stimulator riociguat and the soluble guanylate cyclase activator cinaciguat exert no direct effects on contractility and relaxation of cardiac myocytes from normal rats. Format: AbstractSend to Eur J Pharmaco [3]. Cosyns SM, et al. Influence of cinaciguat on gastrointestinal motility in apo-sGC mice. Neurogastroenterol Motil. 2014 Nov;26(11):1573-85. |