A2AR modulator-1 is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR) with an IC50 value of 9 nM. This compound reduces the affinity of endogenous adenosine for A2aR and inhibits activation of the cAMP signaling pathway. A2AR modulator-1 effectively enhances pCREB phosphorylation in CD4+ T cells, counteracting immunosuppression in the tumor microenvironment. Its ability to suppress tumor growth and metastasis has been demonstrated in models of triple-negative breast cancer, highlighting its potential in cancer research.
A2AR modulator-1 is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR) with an IC50 value of 9 nM. This compound reduces the affinity of endogenous adenosine for A2aR and inhibits activation of the cAMP signaling pathway. A2AR modulator-1 effectively enhances pCREB phosphorylation in CD4+ T cells, counteracting immunosuppression in the tumor microenvironment. Its ability to suppress tumor growth and metastasis has been demonstrated in models of triple-negative breast cancer, highlighting its potential in cancer research.
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