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hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA 2A adenosine receptor (hA 2A AR) antagonist with K i s of 6.4 nM, 4.819 μM, >30 μM for hA 2A AR, hA 1 AR, hA 3 AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with K i s of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.