KW-6356 (Sipagladenant) is a potent and selective adenosine A2A receptor antagonist/inverse agonist with pKi value of9.93 for human A2A receptor.
KW-6356 is a selective ligand for A2A receptor without a high affinity for other neurotransmitter receptors.
KW-6356 exhibits high affinity for A2A receptor in humans, marmosets, dogs, rats, and mice, and high selectivity over the A1, A2B, and A3 receptors in all species.
KW-6356 inhibits CGS21680 induced the concentration-related accumulation of cAMP in Namalwa cells with pKB of 10.00, KW-6356 inhibits the constitutive activity of A2A receptor with pEC50 value of 8.46 in HEK293 cells expressing human A2A receptor.
KW-6356 exerts antagonistic activities and behaves as an insurmountable antagonist, while istradefylline (Cat# PC-42728) acts as a surmountable antagonist.
