化合物Cinaciguat T1984

Product Introduction
Bioactivity


英文名: Cinaciguat

描述: Cinaciguat (BAY 58-2667) 是一种不依赖于一氧化氮的鸟苷酸环化酶化剂，Kd 值为3.2 nM，可用于急性失代偿性心力衰竭的研究。

激酶实验: 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.

体外活性: Cinaciguat (10 μM) significantly enhances intracellular cGMP generation while not having dose-dependent effects on cell contraction and calcium transients[2].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (79.55 mM)


关键字: Inhibitor | inhibit | Cinaciguat | Guanylate Cyclase

相关产品: Vericiguat | Lificiguat | Guanylin (mouse, rat) | Nitroprusside disodium dihydrate | BAY 41-2272 | BAY 41-8543 | Ataciguat | Indusatumab | ODQ | Nelociguat

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | NO PAINS Compound Library

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