SCH442416
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货号：A573317
SCH442416 是一种选择性的腺苷A2A受体拮抗剂。SCH-442416与人类和大鼠A2A受体结合具有高亲和力（Ki值分别为0.048和0.5 nM）。它显示出对hA2A受体的选择性比hA1高出超过23000倍，并且对hA2B和hA3受体的亲和力较低（IC50 > 10 μM）。
SCH442416 化学结构
SCH442416 3D分子结构
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SCH442416 纯度/质量文件 产品仅供科研
货号：A573317
标准纯度：
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产品说明书
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SCH442416 质控信息
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
++
A2AR, Ki: 4 nM
A1R, Ki: 264 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。
SCH442416 生物活性
描述
Adenosine receptors are a family of GPCRs containing four subtypes (A1 , A2A , A2B and A3 receptors), all of which bind the ubiquitous nucleoside adenosine.[1] [2] [3] [4] [5] [6]
SCH442416 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
NCT00531193
Healthy
Phase 1
Completed
-
United Kingdom
... 展开 >> Research Site
London, United Kingdom 收起 <<
NCT02764892
Parkinson's Disease
Phase 1
Completed
-
-
SCH442416 参考文献
[1] Elizabeth A Vecchio,et al. New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism. Br J Pharmacol. 2018 Nov;175(21):4036-4046.
[2] Bruce N Cronstein, et al. Adenosine and adenosine receptors in the pathogenesis and treatment of rheumatic diseases. Nat Rev Rheumatol. 2017. 13(1), 41-51.
[3] Todde S, et, al. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography. J Med Chem. 2000. 43(23), 4359-62.
[4] Moresco RM, et, al. In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. Eur J Nucl Med Mol Imaging. 2005. 32(4), 405-13.
[5] Zheng J, et, al. Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am J Physiol Heart Circ Physiol. 2007 Dec;293(6):H3685-91.
[6] Maimon N, et, al. Pre-exposure to adenosine, acting via A(2A) receptors on endothelial cells, alters the protein kinase A dependence of adenosine-induced dilation in skeletal muscle resistance arterioles. J Physiol. 2014. 592(12), 2575-90.
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SCH442416 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.57mL
0.51mL
0.26mL
12.84mL
2.57mL
1.28mL
25.68mL
5.14mL
2.57mL
SCH442416 技术信息
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