Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 355 | 现货 | ||
2 mg | ¥ 513 | 现货 | ||
5 mg | ¥ 1,070 | 现货 | ||
10 mg | ¥ 1,650 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,480 | 现货 | ||
100 mg | ¥ 6,280 | 现货 | ||
500 mg | ¥ 12,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,330 | 现货 |
产品描述 | 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. |
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]. |
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. |
别名 | BAY 58-2667 |
分子量 | 565.7 |
分子式 | C36H39NO5 |
CAS No. | 329773-35-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (79.55 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7677 mL | 8.8386 mL | 17.6772 mL | 44.193 mL |
5 mM | 0.3535 mL | 1.7677 mL | 3.5354 mL | 8.8386 mL | |
10 mM | 0.1768 mL | 0.8839 mL | 1.7677 mL | 4.4193 mL | |
20 mM | 0.0884 mL | 0.4419 mL | 0.8839 mL | 2.2097 mL | |
50 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8839 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Cinaciguat 329773-35-5 GPCR/G Protein Guanylate cyclase Inhibitor BAY 58-2667 inhibit Guanylate Cyclase inhibitor