|2-(呋喃-2-基)-7-(3-(4-甲氧基苯基)丙基)-7H-吡唑啉[4,3-e][1,2,4]三唑[1,5-c]嘧啶-5-胺|CsnPharm

CAS No.: 316173-57-6

SCH442416 Catalog No. CSN23108

Synonyms: SCH 442416

SCH-442416 is a selective adenosine A2A receptor antagonist. SCH-442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). It displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM).

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400-920-2911

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技术信息

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 ... more >> Research Site London, United Kingdom Collapse <<
NCT02764892	Parkinson's Disease	Phase 1	Completed	-	-

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5680 mL
- 12.8399 mL
- 25.6798 mL
- 5 mM
- 0.5136 mL
- 2.5680 mL
- 5.1360 mL
- 10 mM
- 0.2568 mL
- 1.2840 mL
- 2.5680 mL

技术信息

CAS号

316173-57-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H19N7O2

运输

蓝冰

分子量

389.41

别名

SCH 442416

溶解度

DMSO	78.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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