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(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號 | HY-10171 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥/生物制藥 |
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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(dá)人 Ca2+ 受體的 HEK 293 細(xì)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.
相關(guān)產(chǎn)品：Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Orally Active Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | NPS-2143 | Etelcalcetide hydrochloride | Gadolinium chloride | Cinacalcet | Evocalcet | Calhex 231 hydrochloride | Tecalcet Hydrochloride | γ-L-Glutamyl-L-alanine | NPS 2390 | Ligustroflavone | Upacicalcet sodium | Calcium-Sensing Receptor Antagonists I | SB-423562 | Calindol hydrochloride | GSK3004774 | Strontium Ranelate | AC-265347 | CaSR antagonist-1 | Gamma-Glu-Abu | SB-423557
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