Size | Price | Stock |
---|---|---|
5mg | $60 | In-stock |
10mg | $100 | In-stock |
50mg | $350 | In-stock |
100mg | $560 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-10007 |
M.Wt: | 408.92 |
Formula: | C24H25ClN2O2 |
Purity: | >98 % |
Solubility: | DMSO : 17.86 mg/mL (43.68 mM; ultrasonic and adjust pH to 2 with H2O) |
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 Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor[1][2].
IC50 & Target: IC50: 43 nM (Ca2+ receptor)
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 Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation[1].
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[3]. 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[4].
In Vivo: NPS-2143 (SB-262470A) results in a rapid 4- to 5-fold increase in plasma PTH levels in rats[1].
In normotensive rats, NPS-2143 administration (1 mg/kg, i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands[2].
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