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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 腺苷受体 / Capadenoson/卡帕诺生

Capadenoson/卡帕诺生 {[allProObj[0].p_purity_real_show]}

货号：A146488 同义名： BAY 68-4986

Capadenoson is an oral active, potent and selective adenosine A1 receptor agonist.

Capadenoson/卡帕诺生 化学结构 CAS号：544417-40-5
Capadenoson/卡帕诺生 化学结构
CAS号：544417-40-5
Capadenoson/卡帕诺生 3D分子结构
CAS号：544417-40-5
Capadenoson/卡帕诺生 化学结构 CAS号：544417-40-5
Capadenoson/卡帕诺生 3D分子结构 CAS号：544417-40-5
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Capadenoson/卡帕诺生 纯度/质量文件 产品仅供科研

货号：A146488 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 Adenosine Receptor ↓ 其他靶点 纯度
ZM241385 ✔ 99%+
Istradefylline +++

Adenosine A2A receptor, Ki: 2.2 nM

 		98%
Reversine +

human A3 adenosine receptor, Ki: 0.66 μM

 		98%
SCH58261 ++++

bovine A2a, Ki: 2.0 nM

rat A2a, Ki: 2.3 nM

 		99%+
A2A receptor antagonist 1 ++

A1R, Ki: 264 nM

A2AR, Ki: 4 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Capadenoson/卡帕诺生 生物活性

描述 Adenosine receptor plays important roles in the fertilization process, kidney function and ethanol intoxication as well as angina and heart failure, thus becoming a promising target in clinic. Capadenoson is a selective agonist of adenosine receptor showing Ki of 4.2 nM when binding on rat cortical brain membranes. Capadenoson could also decrease neurotransmitter norepinephrine (NE) releasing at very low concentration. At a concentration of 0.15 mg/kg, capadenoson treatment led to 15% increasing in heart rate during stress[1]. In another investigation, sixty-two male patients with stable angina were studied and treated with capadenoson at oral doses of 1, 2.5, 5, 10 and 20 mg respectively and placebo group was settled as the control. In 10 mg group heart rate was reduced by 12.2 bpm which was 6.8 bpm in 20 mg group in the primary efficacy analysis. Mean HR reduction after dosing for 24 h were 9.9 and 10.3 bpm for 10 mg and 20 mg respectively. In terms of safety, 32% of these patients had suffered at least one adverse events (AE), which was 36%, 30%, 20% and 30% in the control, the 5 mg, 10 mg and 20 mg respevtively, suggesting the 10 mg dose could be the best concentration to reduce heart rate in clinic[2][3].
作用机制 Capadenoson binding to the adenosine-A1 receptor that can inhibit adenylcyclase and decrease cAMP production by activating A1-coupled Gi protein[3] .

Capadenoson/卡帕诺生 动物研究

Dose Rat: 0.03 mg/kg - 0.3 mg/kg[4] (i.v.); 1 mg/kg, 2 mg/kg[5] (i.p.)
Administration i.v., i.p.
Pharmacokinetics
Animal Rats[6] Dogs[6] Monkeys[6]
Dose 0.5 mg/kg (i.v.)
1 mg/kg (p.o.) 		0.3 mg/kg (i.v.)
1 mg/kg (p.o.) 		0.3 mg/kg (i.v.)
1 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o.
F 57% (p.o.) 21% (p.o.) 60% (p.o.)
CLb 1.4 L/h/kg (i.v.) 1.2 L/h/kg (i.v.) 0.21 L/h/kg (i.v.)
T1/2 8.4 h 2.4 h 9.8 h
Vss 10 L/kg (i.v.) 2.3 L/kg 2.7 L/kg

Capadenoson/卡帕诺生 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00568945 Atrial Fibrillation Phase 2 Completed - Germany ... 展开 >> Erfurt, Thüringen, Germany, 99084 收起 <<
NCT00518921 Chronic Stable Angina Phase 2 Withdrawn November 2008 Czech Republic ... 展开 >> Brno, Czech Republic, 656 91 Hodonin, Czech Republic, 695 26 Kromeriz, Czech Republic, 767 55 Olomouc, Czech Republic, 775 20 Ostrava, Czech Republic, 708 52 Plzen, Czech Republic, 30599 Praha 13, Czech Republic, 158 00 Praha 6, Czech Republic, 169 02 Hungary Balatonfured, Hungary, 8230 Kecskemet, Hungary, 6000 Miskolc, Hungary, 3526 Pecs, Hungary, 7624 Zalaegerszeg, Hungary, 8900 Israel Hadera, Israel, 38100 Rehovot, Israel, 76100 Safed, Israel, 13100 Italy Mestre, Venezia, Italy, 30174 Genova, Italy, 16132 Pavia, Italy, 27100 Trieste, Italy, 34100 Poland Bialystok, Poland, 15-276 Gdansk, Poland, 80-952 Gdynia, Poland, 81-519 Katowice, Poland, 40-635 Krakow, Poland, 30-501 Legnica, Poland, 59-220 Lodz, Poland, 91-347 Starogard Gdanski, Poland, 83-200 Szczecin, Poland, 70-111 Warszawa, Poland, 03-401 Wroclaw, Poland, 50-420 Wroclaw, Poland, 50-981 Slovakia Bratislava, Slovakia, 811 04 Bratislava, Slovakia, 813 69 Nitra, Slovakia, 949 01 Nove Zamky, Slovakia, 940 34 收起 <<

Capadenoson/卡帕诺生 参考文献

[1]Bott-Flügel L, Bernshausen A, et al. Selective attenuation of norepinephrine release and stress-induced heart rate increase by partial adenosine A1 agonism. PLoS One. 2011;6(3):e18048.

[2]Elzein E, Zablocki J. A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008;17(12):1901-10.

[3]Tendera M, Bernshausen A, et al. The new oral adenosine A1 receptor agonist capadenoson in male patients with stable angina. Clin Res Cardiol. 2012 Jul;101(7):585-91.

[4]Albrecht-Küpper BE, Leineweber K, et al. Partial adenosine A1 receptor agonists for cardiovascular therapies. Purinergic Signal. 2012 Feb;8(Suppl 1):91-9.

[5]Bailey IR, Laughlin B, et al. Optimization of Thermolytic Response to A1 Adenosine Receptor Agonists in Rats. J Pharmacol Exp Ther. 2017 Sep;362(3):424-430.

[6]Meibom D, Albrecht-Küpper B, et al. Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases. ChemMedChem. 2017 May 22;12(10):728-737.

Capadenoson/卡帕诺生 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.61mL

1.92mL

0.96mL

19.23mL

3.85mL

1.92mL

Capadenoson/卡帕诺生 技术信息

CAS号544417-40-5
分子式C25H18ClN5O2S2
分子量 520.03
SMILES Code N#CC1=C(C2=CC=C(OCCO)C=C2)C(C#N)=C(SCC3=CSC(C4=CC=C(Cl)C=C4)=N3)N=C1N
MDL No. MFCD09954113
别名 BAY 68-4986
运输蓝冰
InChI Key CITWCLNVRIKQAF-UHFFFAOYSA-N
Pubchem ID 9936489
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案二

Tags: Capadenoson | 544417-40-5 | BAY 68-4986 | Adenosine Receptor | Adenosine Receptor Agonist | GPCR/G Protein | Adenosine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Capadenoson/卡帕诺生 纯度/质量文件 | Capadenoson/卡帕诺生 亚型比较 | Capadenoson/卡帕诺生 生物活性 | Capadenoson/卡帕诺生 动物研究 | Capadenoson/卡帕诺生 临床数据 | Capadenoson/卡帕诺生 参考文献 | Capadenoson/卡帕诺生 实验方案 | Capadenoson/卡帕诺生 技术信息

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