目錄:MedChemExpress LLC>>信號通路>> NPS-2143 | MedChemExpress (MCE)
| CAS | 284035-33-2 | 純度 | 99.33% |
|---|---|---|---|
| 分子量 | 408.92 | 分子式 | C??H??ClN?O? |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號 | HY-10007 | 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產業(yè),制藥/生物制藥 |
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CAS No. : 284035-33-2
MCE 國際站：NPS-2143
產品活性：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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