"目录号: HY-14181
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。
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
Bayer
Congestive Heart Failure
December 2007
Phase 2
Bayer
Acute Heart Failure
March 2010
Phase 2
Bayer
Heart Failure-Heart Decompensation
April 2010
Phase 2
Bayer
Acute Heart Failure
March 2010
Phase 2
Bayer
Congestive Heart Failure
December 2007
Phase 2
Bayer
Acute Heart Failure
March 2010
Phase 2
Bayer
Heart Failure-Heart Decompensation
April 2010
Phase 2
Bayer
Acute Heart Failure
March 2010
Phase 2
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References
