a-2aar

A2AAR antagonist 3 is a potent and selective A2A adenosine receptor (A2AAR) antagonist with an IC50 value of 1.57 nM. It exhibits a high binding affinity specifically for A2AAR. In vitro studies demonstrate its good stability in rat liver microsomes, and it possesses acceptable pharmacokinetic properties in vivo. A2AAR antagonist 3 is applicable for cancer research.

A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors.

A2AAR antagonist 1 (compound 21a) is a potent A2AAR (adenosine A2A receptor) antagonist with high ligand efficiency and a Ki value of 20 nM. It is applicable in neurodegenerative disease research [1].

A2AAR/HDAC-IN-1 (compound 14c) is an orally active, balanced dual inhibitor of A2AAR (Ki: 163.5 nM) and HDAC1 (IC50: 145.3 nM).

A2AAR/HDAC-IN-2 is a potent dual A2AAR/HDAC inhibitor with good affinity for A2AAR (Ki: 10.3 nM) and effective HDAC1 inhibition (IC50: 18.5 nM). A2AAR/HDAC-IN-2 is applicable in anti-tumour studies.

3′-Methoxyfurano[4″,5″:3,4]chalcone (Compound 2) is a selective A2AAR antagonist with an IC50 of 33.5 nM, indicating it has a high affinity. This compound is a natural product that can be extracted from the skins of Allium cepa L. Additionally, 3′-Methoxyfurano[4″,5″:3,4]chalcone is capable of promoting T cell activation and is useful in cancer immunology research.

Compound 4a, also known as hA2AAR antagonist 1, is a highly selective hA2AAR antagonist with a Ki value of 5 nM. It is useful in the field of immuno-oncology research.