SCH 58261

SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively[1][2][3].

Product Specifications

CAS Number

[160098-96-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/SCH-58261.html

Purity

99.71

Solubility

DMSO : ≥ 34 mg/mL

Smiles

NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14

Molecular Formula

C18H15N7O

Molecular Weight

345.36

Precautions

H302, H315, H319, H335

References & Citations

[1]Zocchi C, et al. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. Br J Pharmacol. 1996 Apr;117 (7) :1381-6.|[2]Varani K, et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117 (8) :1693-701.|[3]Xi J, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009 Nov;47 (5) :684-90.|[4]Kuzumaki N, et al. Multiple analyses of G-protein coupled receptor (GPCR) expression in the development of gefitinib-resistance in transforming non-small-cell lung cancer. PLoS One. 2012;7 (10) :e44368.|[5]Mediavilla-Varela M, et al. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Cancer Biol Ther. 2013 Sep;14 (9) :860-8.|[6]Wardas J, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Brain Res. 2003 Jul 11;977 (2) :270-7.|[7]Wardas J, et al. SCH 58261, an A (2A) adenosine receptor antagonist, counteracts parkinsonian-like muscle rigidity in rats. Synapse. 2001 Aug;41 (2) :160-71.