DS69910557 is a potent, selective and orally activehuman paratroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM. DS69910557 can be used for the research of perparatroidism, percalcemia of malignancy and osteoporosis.
DS69910557 (compound 19e) has highly potent antagonistic activity for PTHR1 with an IC50 value of 0.08 μM[1].DS69910557 (3 μM) exhibits excellent selectivity against human ether-a-go-go-related-gene (hERG) channel[1].
DS69910557 (compound 19e) (p.o.; 5mg/kg) has potency to decrease the plasma calcium concentration in rats in vivo[1].
References:
[1]. Yoshikazu Arai, et al. Lead optimization of pyrido[2,3-d][1]benzazepin-6-one derivatives leading to the discovery of a potent, selective, and orally available human paratroid hormone receptor 1 (hPTHR1) antagonist (DS69910557). Bioorg Med Chem. 2022 Jun 15;64:116763.