A selective, potent inhibitor of PHD2 (IC50 = 1.6 nM); active in vivo, inhibiting prolyl hydroxylation and increasing HIF1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF1α and HIF2α expression in mice; penetrates the blood-brain barrier to induce HIF expression in the brain.