SCH 58261

160098-96-4

C18H15N7O

DMSO : >= 34 mg/mL (98.45 mM)

GPCR/G Protein

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]. IC50 & Target: IC50: 15 nM (A2A receptor)^[2] In Vitro: SCH 58261 (0 nM–10 uM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975^[4].
SCH58261 (25 uM; 72 hours) can inhibit the growth of CAF cells^[5].
In Vivo: SCH 58261 (2 mg/kg; i.p.; daily; for 20 days) causes a decrease in the tumor burden in a NSCLC mouse model^[5].
SCH 58261 (5 mg/kg; i.p.; 3 times; every 3 hours; 10 minutes before haloperidol) partially decreases the haloperidol-induced catalepsy and the increase in the PENK mRNA expression in both dorsolateral and ventrolateral parts of the striatum at all three examined levels^[6].
SCH 58261 diminishes the parkinsonian-like muscle rigidity and potentiates the effect of L-DOPA in rat model^[7].