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SCH442416

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Chemical Structure| 316173-57-6 同义名 : -
CAS号 : 316173-57-6
货号 : A573317
分子式 : C20H19N7O2
纯度 : 99%+
分子量 : 389.411
MDL号 : MFCD08703126
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(154.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]. Adenosine is a potent regulator of inflammation. Adenosine mediates its effects on inflammatory cells by engaging one or more cell-surface receptors[2]. SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively[3]. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). It can be used for imaging of adenosine A2A receptors in rat and primate brain[4]. SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[5]. SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[6].
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 - -
实验方案
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
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.