PCO371是一种可口服的甲状旁腺激素受体1(PTHR1)的完全抑制剂，对PTHR2无作用。
PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor. PCO371 induces cAMP production with an EC50 of 2.4 μM in COS-7 cells expressing hPTHR1, and 2.5 μM in COS-7 cells transfected with hPTHR1-delNT, and also enhances the phospholipase C activity (EC50, 17 μM)[1].
[1]. Tamura T, et al. Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism. Nat Commun. 2016 Nov 18;7:13384.
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