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NPS-2143

CAS No. : 284035-33-2

MCE 國際站：NPS-2143

產(chǎn)品活性：NPS-2143 (SB-262470A)，口服活性溶鈣劑， 是選擇性的鈣敏感受體 (CaSR) 拮抗劑。NPS-2143 (SB-262470A) 阻斷通過激活表達人 Ca²⁺ 受體的 HEK 293 細胞中的 Ca²⁺ 受體而引起的胞漿 Ca²⁺ 濃度增加 (IC₅₀=43 nM)。

研究領(lǐng)域：GPCR/G Protein

作用靶點：CaSR

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.
?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.

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.

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