SCH 58261

• UNSPSC Description:

  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].

• Target Antigen:

  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 Weight:

  345.36

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 3

• CAS Number:

  160098-96-4