目錄:MedChemExpress LLC>>信號通路>> NPS-2143 hydrochloride | MedChemExpress (MCE)
CAS | 324523-20-8 | 純度 | 99.80% |
---|---|---|---|
分子量 | 445.38 | 分子式 | C??H??Cl?N?O? |
供貨周期 | 現貨 | 規格 | 10 mM * 1 mL |
貨號 | HY-10171 | 應用領域 | 醫療衛生,化工,生物產業,制藥 |
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CAS No. : 324523-20-8
MCE 國際站:NPS-2143 hydrochloride
產品活性: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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