NPS-2143 284035-33-2

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Molecular Weight:

408.92 NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM.

Biological Activity

NPS 2143 blocks increases in cytoplasmic Ca2+ concentrations with IC50 of 43 nM elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. NPS 2143 stimulates parathyroid hormone (PTH) secretion from bovine
parathyroid cells with EC50 of 41 nM.


Moreover, NPS 214 also blocks the
inhibitory effects of calcimimetic NPS R-467 on PTH secretion from
bovine parathyroid cells and the inhibitory effects of extracellular
Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation.


In HEK-293 cells transiently expressing hCaSRs, NPS 2143 significantly
suppresses the kokumi taste by effectively inhibiting the activity of
both GSH (data not shown) and γ-Glu-Val-Gly. A recent
study shows that NPS 2143 treatment suppresses low molecular weight
fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion
in CaSR-transfected HEK 293 cells.


In rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels. In normotensive rats, NPS 2143 administration (1 mg/kg) by i.v.
markedly increases mean arterial blood pressure (MAP) in the presence of
parathyroid glands.

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Product Categories : GPCR & G Protein > CaSR Inhibitor