A2A receptor antagonist 3

Names

[ CAS No. ]:
2738606-83-0

[ Name ]:
A2A receptor antagonist 3

Biological Activity

[Description]:

A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[Target]

A2AR:0.4 nM (Ki)

A2BR:37 nM (Ki)

A1R:107 nM (Ki)

A3R:1467 nM (Ki)


[In Vitro]

A2A receptor antagonist 3 (Example 92) (24 h) inhibits CD3/CD28 stimulated IL-2 release with an IC50 of 0.004 μM[1]. A2A receptor antagonist 3 (20 min) inhibits pCREB in CD8+T cells in human whole blood with an IC50 of 0.02 μM[1].

[References]

[1]. Clive Mccarthy, et al. Antagonists of the adenosine a2a receptor. Patent WO2021224636 A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H26N6O2

[ Molecular Weight ]:
454.52

Related Compounds