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Capadenoson

Capadenoson

产品编号 TQ0125   CAS 544417-40-5
别名: BAY 68-4986, 卡帕诺生

Capadenoson (BAY 68-4986) 是 A1 腺苷受体的选择性激动剂。

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Capadenoson Chemical Structure
Capadenoson, CAS 544417-40-5
规格 价格/CNY 货期 数量
1 mg ¥ 233 现货
5 mg ¥ 536 现货
10 mg ¥ 829 现货
25 mg ¥ 1,590 现货
50 mg ¥ 2,380 现货
1 mL * 10 mM (in DMSO) ¥ 686 现货
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
MG-132限时半价
产品目录号及名称: Capadenoson (TQ0125)
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选择批次  
纯度: 99.62%
纯度: 98.85%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Capadenoson (BAY 68-4986) is a selective adenosine-A1 receptor agonist.
体外活性 为了进一步阐明Capadenson的药理特性,采用标准全A1激动剂CCPA和A1拮抗剂DPCPX进行GTP转移试验。在大鼠皮质脑膜结合实验中,CCPA显示出4.2 nM的Ki值。在1 mM GTP存在下,该Ki值转变为64 nM,因此,CCPA的GTP转移值为15。DPCPX在GTP存在与否下显示出几乎相同的Ki值,其GTP转移值为1。Capadenson在结合实验中显示出24 nM的Ki值,在1 mM GTP存在下,该Ki值转变为116 nM,从而得出Capadenson的GTP转移值为5。
体内活性 在活体实验中,Wistar大鼠和SHR在进行应激测试(体力限制)的前5天预先用Capadenoson(0.15 mg/kg)处理。在第5天,进行为期2小时的应激测试。在限制应激测试前的5天内,Capadenoson的血浆浓度在服药后3小时测量,保持恒定,第4天和第5天的平均浓度分别为7.63 μg/L。
激酶实验 Membranes from the human cortex are prepared. [35S]GTPγS binding is measured. Briefly, 5 μg of membrane protein is incubated in a total volume of 160 μL for 2 hr at 25°C in a shaking water bath. [35S]GTPγS binding in control incubations and in the presence of Capadenoson showed a linear time course up to this incubation time. Binding buffer contained 50 mM Tris/HCl, pH 7.4, 2 mM triethanolamine, 1 mM EDTA, 5 mM MgCl2, 10 μM GDP, 1 mM dithiothreitol, 100 mM NaCl, 0.2 units/mL adenosine deaminase, 0.2 nM [35S]GTPγS, and 0.5% bovine serum albumin. Non-specific binding is determined in the presence of 10 μM GTPγS. Incubations are terminated through filtration of the samples over multiscreen FB glass fiber filters followed by two washes with binding buffer. The filters are dried, coated with scintillator and counted for radioactivity. Binding curves of [35S]GTPγS are analyzed by nonlinear regression using GraphPad Prism.
动物实验 A total of 14 Wistar rats and 18 SHR (bodyweight 200-50 g, all-female) underwent experiments to evaluate the exocytotic, stimulation-induced NE release during electrical field stimulation. Rats are killed by an injection of pentobarbital i.p. (0.5 mL/100 mg body weight), and hearts are rapidly excised, and placed in ice-cold Krebs-Henseleit solution (KHL). They are quickly mounted on a Langendorff apparatus for retrograde perfusion with KHL. Perfusion rate is kept constant at 10 mL/min, the temperature is adjusted to 37°C, and the pH to 7.4 through bubbling with 5% CO2/95% O2. Via an inflow line desipramine at a concentration of 10?7 M is added to the perfusion buffer. After an equilibration period of 20 minutes, electrical field stimulation is commenced via two metal paddles adjacent to both sides of the beating heart for 1 minute (5V, 6 Hz). We collected the efflux in plastic tubes the minute before, during, and 3 minutes after the stimulation. These are rapidly frozen in liquid nitrogen and stored at ?20°C till analysis. The NE release is calculated as the cumulative release induced by electrical stimulation. After the first stimulation (S1), the study drug Capadenoson at concentrations of 30 μg/L (6×10^?8 M) or 300 μg/L(6×10^?7 M), or CCPA (10^?6 M), respectively, are added via separate perfusion lines for 30 minutes. After this time a second stimulation (S2) is executed to determine the effect of the drugs on NE release compared to the first stimulation. The effect of each pharmacological intervention is analyzed by calculating the ratio of NE release induced by the second and first stimulation (S2/S1 ratio).
别名 BAY 68-4986, 卡帕诺生
分子量 520.03
分子式 C25H18ClN5O2S2
CAS No. 544417-40-5

存储

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

溶解度

DMSO: 50 mg/mL (96.15 mM)

H2O: Insoluble

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 1.923 mL 9.6148 mL 19.2297 mL 48.0741 mL
5 mM 0.3846 mL 1.923 mL 3.8459 mL 9.6148 mL
10 mM 0.1923 mL 0.9615 mL 1.923 mL 4.8074 mL
20 mM 0.0961 mL 0.4807 mL 0.9615 mL 2.4037 mL
50 mM 0.0385 mL 0.1923 mL 0.3846 mL 0.9615 mL

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TargetMol Library Books参考文献

1. Bott-Flügel L, et al. Selective attenuation of norepinephrine release and stress-induced heart rate increase by partial adenosine A1 agonism. PLoS One. 2011 Mar 28;6(3):e18048.
AZD4635 PD 117519 Tozadenant A2AR-agonist-1 MRS1220 Inosine KFM19 Taminadenant

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗癌临床化合物库 抗癌药物库 GPCR靶点分子库 抗心血管疾病化合物库 ReFRAME 相关化合物库 NO PAINS 化合物库 已知活性化合物库 经典已知活性库 神经信号分子库

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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

Capadenoson 544417-40-5 GPCR/G Protein Neuroscience Adenosine Receptor P1 receptor Inhibitor inhibit BAY 68-4986 卡帕诺生 inhibitor

 

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