A2AR modulator-1

A2AR modulator-1 (Compound 45) is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR), with an IC50 value of 9 nM. It reduces the affinity of endogenous adenosine for the receptor and inhibits the activation of the cAMP signaling pathway. A2AR modulator-1 effectively restores pCREB phosphorylation in CD4+ T cells, reverses immunosuppression in the tumor microenvironment, and shows potential in inhibiting tumor growth and metastasis in a triple-negative breast cancer model.