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.

Cinaciguat（10 μM）显著增强细胞内cGMP生成，同时对细胞收缩和钙瞬变没有剂量依赖性影响[2]。

Cinaciguat (10 mg/kg/天, p.o.) 在糖尿病大鼠中的治疗不会影响血糖水平，同时能够减少水摄入量。Cinaciguat治疗能够缓解糖尿病相关的氧化应激，保护免受DM相关NO-sGC-cGMP-PKG信号途径的改变，同时减轻糖尿病相关的心肌肥厚和凋亡[1]。Cinaciguat（1-10-100 nM）在WT和apo-sGC小鼠的条带中诱导浓度依赖性的松弛，但对由PGF2α在WT或apo-sGC条带中诱导的相位活动没有任何影响[3]。

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.