MedChemExpress - Model SCH442416 -316173-57-6
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. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain[1][2].MCE products for research use only. We do not sell to patients.
SCH442416
MCE China：SCH442416
Brand：MedChemExpress (MCE)
Cat. No.HY-103169
CAS：316173-57-6
Purity：99.68%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
In Vitro：SCH442416 is selective for A2AR (Ki=0.50 nM) in rat striatal membranes over A1R and A3R (Ki=1815 and >10000, respectively)[1]. SCH442416 (0.1-10?μM) increases the glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) proteins expression of Müller cells in Group 1?μM[5].
In Vivo：SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[3]. SCH-442416 (1 μM?2μL; i.v.) increases the GS and GLAST protein expression in rats[5]. SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[4].
IC50 & Target：IC50: 0.048 nM (hA2AR), 0.5 nM (rA2AR)[1] In Vitro SCH442416 is selective for A2AR (Ki=0.50 nM) in rat striatal membranes over A1R and A3R (Ki=1815 and >10000, respectively)[1]. SCH442416 (0.1-10?μM) increases the glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) proteins expression of Müller cells in Group 1?μM[5]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SCH442416 Related Antibodies
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References：
[1]. 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 Nov 16;43(23):4359-62. [Content Brief]
[2]. 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 Apr;32(4):405-13. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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 Jun 15;592(12):2575-90. [Content Brief]
[5]. Yu J, et, al. A 2A R Antagonists Upregulate Expression of GS and GLAST in Rat Hypoxia Model. Biomed Res Int. 2020 Oct 26;2020:2054293. [Content Brief]
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