| Name | Cinaciguat |
| Description | Cinaciguat (BAY 58-2667) (BAY 58-2667) is the first of a new class of soluble guanylate cyclase (sGC) activators in Clinicalal development for acute decompensated heart failure. |
| 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. |
| In vitro | Cinaciguat (10 μM) significantly enhances intracellular cGMP generation without exhibiting 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 affect blood glucose levels but reduces water intake, alleviates diabetes mellitus-related oxidative stress, protects against alterations in the NO-sGC-cGMP-PKG signaling pathway, and reduces 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 influence phasic activity induced by PGF2α in WT or apo-sGC strips[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (79.55 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2 mg/mL (3.54 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | Guanylatecyclase | guanylate cyclase | Cinaciguat |
| Inhibitors Related | LY83583 | Lificiguat | Zagociguat | Sinitrodil | NPR-C activator 1 | Riociguat | Nelociguat | Nitroprusside disodium dihydrate | NS-2028 | Indusatumab | Methylene Blue | Methylene Blue trihydrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Obesity Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
