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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-SCH-442416
SCH-442416

Chemical Structure : SCH-442416

CAS No.: 316173-57-6

SCH-442416 (SCH442416 )

货号: PC-20110Not For Human Use, Lab Use Only.

SCH-442416 (SCH442416) is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR) with Ki 0.048 nM and 0.5 nM for human and rat A2AR, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SCH-442416 (SCH442416) is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR) with Ki 0.048 nM and 0.5 nM for human and rat A2AR, respectively.
SCH-442416 displays >23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively).
SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.
SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury.

物理化学性质&存储条件

分子量 389.42
分子式 C20H19N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-Furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine

参考文献

1. Todde S, et al. J Med Chem. 2000 Nov 16;43(23):4359-62.

2. Rahimian R, et al. Eur J Pharmacol. 2010 Dec 15;649(1-3):376-81.

3. Kumar TS, et al. Bioorg Med Chem Lett. 2011 May 1;21(9):2740-5.

4. Orrú M, et al. Neuropharmacology. 2011 Oct-Nov;61(5-6):967-74.

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