"目录号: HY-14181
GPCR/G Protein-
Cinaciguat 是一种鸟苷酸环化酶(guanylate cyclase) 激活剂，用于治疗急性失代偿性心力衰竭。
Guanylate Cyclase
相关产品
Lificiguat-Riociguat-Linaclotide-BAY 41-2272-Cinaciguat hydrochloride-Vericiguat-
生物活性
Description
Cinaciguat is an activator ofguanylate 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 PGF2αin WT or apo-sGC strips[3].
Clinical Trial
NCT00559650
Bayer
Congestive Heart Failure
December 2007
Phase 2
NCT01067859
Bayer
Acute Heart Failure
March 2010
Phase 2
NCT01064037
Bayer
Heart Failure-Heart Decompensation
April 2010
Phase 2
NCT01065077
Bayer
Acute Heart Failure
March 2010
Phase 2
NCT00559650
Bayer
Congestive Heart Failure
December 2007
Phase 2
NCT01067859
Bayer
Acute Heart Failure
March 2010
Phase 2
NCT01064037
Bayer
Heart Failure-Heart Decompensation
April 2010
Phase 2
NCT01065077
Bayer
Acute Heart Failure
March 2010
Phase 2
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References
[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.