2. GPCR/G Protein
  3. Adenosine Receptor
  4. Capadenoson

Capadenoson  (Synonyms: BAY 68-4986)

目录号: HY-14917 纯度: 99.62%
COA 产品使用指南

摩尔计算器

Capadenoson 是一种选择性的腺苷-A1受体 (adenosine-A1 receptor) 激动剂。

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Capadenoson Chemical Structure

Capadenoson Chemical Structure

CAS No. : 544417-40-5

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规格 价格 是否有货 数量
10 mM * 1ML in DMSO ￥669
In-stock
5 mg ￥585
In-stock
10 mg ￥877
In-stock
25 mg ￥1755
In-stock
50 mg ￥2633
In-stock
100 mg ￥3950
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Capadenoson 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Capadenoson is a selective agonist of adenosine-A1 receptor.

IC50 & Target

Adenosine A1 receptor[1]
体外研究
(In Vitro)

To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Capadenoson 相关抗体:
体内研究
(In Vivo)

In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

520.03

Formula

C25H18ClN5O2S2
CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

卡帕诺生
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 50 mg/mL (96.15 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9230 mL 9.6148 mL 19.2297 mL
5 mM 0.3846 mL 1.9230 mL 3.8459 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.81 mM); 悬浊液; 超声加热助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.81 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.62%

COA (284 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
A total of 14 Wistar rats and 18 SHR (body weight 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 the 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 2-chloro-N6-cyclopentyladenosine (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 analysed by calculating the ratio of NE release induced by the second and first stimulation (S2/S1 ratio).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Capadenoson 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9230 mL 9.6148 mL 19.2297 mL 48.0741 mL
5 mM 0.3846 mL 1.9230 mL 3.8459 mL 9.6148 mL
10 mM 0.1923 mL 0.9615 mL 1.9230 mL 4.8074 mL
15 mM 0.1282 mL 0.6410 mL 1.2820 mL 3.2049 mL
20 mM 0.0961 mL 0.4807 mL 0.9615 mL 2.4037 mL
25 mM 0.0769 mL 0.3846 mL 0.7692 mL 1.9230 mL
30 mM 0.0641 mL 0.3205 mL 0.6410 mL 1.6025 mL
40 mM 0.0481 mL 0.2404 mL 0.4807 mL 1.2019 mL
50 mM 0.0385 mL 0.1923 mL 0.3846 mL 0.9615 mL
60 mM 0.0320 mL 0.1602 mL 0.3205 mL 0.8012 mL
80 mM 0.0240 mL 0.1202 mL 0.2404 mL 0.6009 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Capadenoson544417-40-5BAY 68-4986卡帕诺生Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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