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DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR).1 It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.
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1. Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-