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Cinaciguat

Catalog No. T1984 CAS 329773-35-5

Synonyms: BAY 58-2667

Cinaciguat (BAY 58-2667) is the first of a new class of soluble guanylate cyclase (sGC) activators in Clinicalal development for acute decompensated heart failure.

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Cinaciguat, CAS 329773-35-5

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Purity: 98%

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Description	Cinaciguat (BAY 58-2667) is the first of a new class of soluble guanylate cyclase (sGC) activators in Clinicalal development for acute decompensated heart failure.
In vitro	Cinaciguat (10 μM) significantly enhances intracellular cGMP generation while not having 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 while leading 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].
Kinase Assay	HDAC Inhibition Assays: Purified HDACs are incubated with 1 mM carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25 °C in HDAC assay buffer containing 100 mM HEPES (pH 7.5), 25 mM KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model: ((A+((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve. The standard errors of the IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the formula xf4_FitResultStdError.

Synonyms	BAY 58-2667
Molecular Weight	565.71
Formula	C36H39NO5
CAS No.	329773-35-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. The soluble guanylate cyclase activator cinaciguat prevents cardiac dysfunction in a rat model of type-1 diabetes mellitus[J]. Cardiovascular Diabetology, 2015, 14(1):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.

Citations

1. Liu R, Kang Y, Chen L. Activation mechanism of human soluble guanylate cyclase by stimulators and activators. Nature Communications. 2021, 12(1): 1-10.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Cardiovascular Disease Compound Library Drug Repurposing Compound Library Anti-COVID-19 Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Clinical Compound Library

Related Products

Related compounds with same targets

Plecanatide Nelociguat Nitroprusside disodium dihydrate Methylene Blue MCUF-651 LY83583 ODQ Runcaciguat

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Keywords

Cinaciguat 329773-35-5 G蛋白偶联受体 Guanylate cyclase Inhibitor inhibit Guanylate Cyclase BAY 58-2667 inhibitor

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