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Capadenoson
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Capadenoson图片
CAS NO:544417-40-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
卡帕诺生
BAY 68-4986
产品介绍
CaPADeNOSon 是 A1 腺苷受体的选择性激动剂。

产品描述

Capadenoson is a selective adenosine-A1 receptor agonist.

体外活性

To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist DPCPX. CCPA shows a Ki value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki values in the absence and presence of GTP. Capadenson shows a Ki value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson.

体内活性

In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson (0.15 mg/kg) for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 μg/L on day 4 and 5, respectively.

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).

Cas No.

544417-40-5

分子式

C25H18ClN5O2S2

分子量

520.03

别名

卡帕诺生;BAY 68-4986

储存和溶解度

H2O:Insoluble
DMSO:50 mg/mL (96.15 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years