1. GPCR/G Protein
  2. Adenosine Receptor
  3. Tecadenoson

Tecadenoson  (Synonyms: CVT-510)

目录号: HY-19661 纯度: 99.76%
COA 产品使用指南

Tecadenoson (CVT-510) 是选择性的腺苷受体 (A1 adenosine receptor) 激动剂。

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Tecadenoson Chemical Structure

Tecadenoson Chemical Structure

CAS No. : 204512-90-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3190
In-stock
5 mg ¥2900
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10 mg ¥4600
In-stock
25 mg ¥9200
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50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.

IC50 & Target

Target: A1 adenosine receptor[1]

体外研究
(In Vitro)

In the atrial-paced isolated heart, Tecadenoson is approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50=41 nM) than to increase coronary conductance (EC50=200 nM). At concentrations of Tecadenoson (40 nM) and diltiazem (1 μM) that causes equal prolongation of S-H interval (∼10 ms), diltiazem, but not Tecadenoson, significantly reduces left ventricular developed pressure (LVP) and markedly increases coronary conductance. Tecadenoson shortens atrial (EC50=73 nM) but not the ventricular monophasic action potentials (MAP)[1].

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

体内研究
(In Vivo)

In atrial-paced anaesthetized guinea-pigs, intravenous infusions of Tecadenoson and diltiazem causes nearly equal prolongations of P-R interval[1]. Tecadenoson (2, 5, 20 μg/kg i.p.) causes a rapid and sustained dose-dependent decrease in NEFA at doses that do not cause bradycardia. Tecadenoson given at 50 μg/kg causes a significant bradycardia (50% decrease in heart rate at 25 min[2].

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

Clinical Trial
分子量

337.33

Formula

C14H19N5O5

CAS 号
性状

固体

颜色

White to off-white

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
In Vitro: 

DMSO 中的溶解度 : 200 mg/mL (592.89 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9645 mL 14.8223 mL 29.6446 mL
5 mM 0.5929 mL 2.9645 mL 5.9289 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

In Vivo:

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: ≥ 5 mg/mL (14.82 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (14.82 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

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
参考文献
Kinase Assay
[1]

The effect of Tecadenoson on binding to A1 and A2A-adenosine receptors of porcine forebrain and striatum membranes, respectively, are determined. Assays for A1 and A2A receptors are carried out by using the A1 receptor antagonist [3H]CPX and the A2A receptor agonist [3H]CGS 21680. Membranes are treated with adenosine deaminase (2 U/mL) for 20 min at room temperature prior to and during radioligand binding assays. Membranes (0.2-0.7 mg), adenosine deaminase, and the indicated radioligand are incubated for 3 h in a 300 μL volume of Tris-HCl buffer (50 mM) (pH 7.4). Assays are carried out in triplicate at room temperature. After the incubation period, bound and free radioligand are diluted by the addition of ice-cold Tris-HCl buffer (5 mL), and immediately separated by vacuum filtration of assay contents onto Whatman GF/C filters and ishing of trapped membranes with Tris-HCl buffer (20 mL). Filter disks containing membrane-bound radioactivity are placed in 4 mL Scintiverse, and the radioactivity is quantified by a liquid scintillation counter. Specific binding of [3H]CPX and [3H]CGS 21680 is defined as membrane binding displaced in the presence of CPT (10 μM) and R-PIA (10 μM), respectively[1].

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

Animal Administration
[2]

Rat: The effects of Tecadenoson on heart rate and to reduce serum NEFA concentration are determined in separate groups of rats to avoid the effects of animal handling and blood sampling on heart rate. Three days before an experiment, a catheter (0.025-mm outer diameter) is implanted in the left common carotid artery of each rat using aseptic conditions and sterile technique. The catheter is tunneled subcutaneously to the dorsal surface. After recovery from anesthesia, rats are placed in metabolic cages to facilitate handling and blood sampling. Blood samples (0.2 mL) are drawn before and at various time points after i.p. injection of either Tecadenoson or vehicle (DMSO in saline). A 0.4-mL volume of 1% sodium citrate in saline is administered after withdrawal of each blood sample to replace blood volume and prevent clotting in the carotid artery catheter. Serum is collected from each sample after centrifugation of the clotted blood. Serum samples are stored at −80°C until analysis. Serum NEFA concentration is determined using an enzymatic colorimetric assay kit[2].

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

参考文献

Tecadenoson 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 2.9645 mL 14.8223 mL 29.6446 mL 74.1114 mL
5 mM 0.5929 mL 2.9645 mL 5.9289 mL 14.8223 mL
10 mM 0.2964 mL 1.4822 mL 2.9645 mL 7.4111 mL
15 mM 0.1976 mL 0.9882 mL 1.9763 mL 4.9408 mL
20 mM 0.1482 mL 0.7411 mL 1.4822 mL 3.7056 mL
25 mM 0.1186 mL 0.5929 mL 1.1858 mL 2.9645 mL
30 mM 0.0988 mL 0.4941 mL 0.9882 mL 2.4704 mL
40 mM 0.0741 mL 0.3706 mL 0.7411 mL 1.8528 mL
50 mM 0.0593 mL 0.2964 mL 0.5929 mL 1.4822 mL
60 mM 0.0494 mL 0.2470 mL 0.4941 mL 1.2352 mL
80 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9264 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7411 mL
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  • 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.

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目录号:
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