NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca concentrations (IC50=43 nM) elicited by activating the Ca receptor in HEK 293 cells expressing the human Ca receptor.
性状
Solid
IC50 & Target[1][2]
IC50: 43 nM (Ca receptor)
体外研究(In Vitro)
NPS-2143 (SB-262470A) 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 Ca 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 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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
NPS-2143 (SB-262470A) results in a rapid 4- to 5-fold increase in plasma PTH levels in rats.
In normotensive rats, NPS-2143 administration (1 mg/kg, i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.