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Cinaciguat

Cinaciguat

产品编号 T1984   CAS 329773-35-5
别名: BAY 58-2667

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。

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Cinaciguat Chemical Structure
Cinaciguat, CAS 329773-35-5
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
其他形式的 Cinaciguat:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Cinaciguat (T1984)
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纯度: 99.82%
纯度: 99.18%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

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

溶解度

DMSO: 45 mg/mL (79.55 mM)

溶液配制表

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

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TargetMol Library Books参考文献

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.

TargetMol Library Books文献引用

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.
Glutaminyl Cyclase Inhibitor 1 Vericiguat Ataciguat Guanylin (mouse, rat) Methylene Blue trihydrate BAY 41-2272 Sinitrodil Uroguanylin (human)

相关化合物库

该产品包含在如下化合物库中:
GPCR靶点分子库 抗癌临床化合物库 药物功能重定位化合物库 抗癌药物库 已知活性化合物库 抗COVID-19化合物库 经典已知活性库 人代谢物化合物库 临床期小分子药物库 NO PAINS 化合物库

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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。

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Keywords

Cinaciguat 329773-35-5 GPCR/G Protein Guanylate cyclase Inhibitor BAY 58-2667 inhibit Guanylate Cyclase inhibitor

 

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