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KW-6356

Chemical Structure : KW-6356

CAS No.: 858979-50-7

KW-6356 (KW6356, Sipagladenant)

Catalog No.: PC-20102Not For Human Use, Lab Use Only.

KW-6356 (Sipagladenant) is a potent and selective adenosine A2A receptor antagonist/inverse agonist with pKi value of9.93 for human A2A receptor.

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Biological Activity

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.

Physicochemical Properties

M.Wt 397.45
Formula C20H19N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[4-(furan-2-yl)-5-(oxane-4-carbonyl)-1,3-thiazol-2-yl]-6-methylpyridine-3-carboxamide

References

1. Ohno Y, et al. Mol Pharmacol. 2023 Mar 9:MOLPHARM-AR-2022-000633.

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