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NPS-2143 hydrochloride

CAS No. : 324523-20-8

MCE 國際站：NPS-2143 hydrochloride

產(chǎn)品活性：NPS-2143 hydrochloride (SB-262470A hydrochloride)，口服活性溶鈣劑，是選擇性的鈣敏感受體 (CaSR) 拮抗劑。NPS-2143 hydrochloride (SB-262470A hydrochloride) 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 hydrochloride (SB-262470A hydrochloride) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC₅₀ of 41 nM. Moreover, NPS-2143 hydrochloride 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 Vivo: When infused intravenously in normal rats, NPS-2143 hydrochloride (SB-262470A hydrochloride) causes a rapid and large increase in plasma levels of PTH. Ca²⁺ receptor antagonists are termed calcilytics and NPS-2143 is the first substance (either atomic or molecular) shown to possess such activity.
When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats.

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