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NPS-2143 hydrochloride

CAS No. : 324523-20-8

MCE 站：NPS-2143 hydrochloride

产品活性：NPS-2143 hydrochloride (SB-262470A hydrochloride)，口服活性溶钙剂，是选择性的钙敏感受体 (CaSR) 拮抗剂。NPS-2143 hydrochloride (SB-262470A hydrochloride) 通过激活表达人 Ca²⁺ 受体的 HEK 293 细胞中的 Ca²⁺ 受体而引起的胞浆 Ca²⁺ 浓度增加 (IC₅₀=43 nM)。

研究领域：GPCR/G Protein

作用靶点：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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Orally Active Compound Library  |  NPS-2143  |  Cinacalcet  |  Tecalcet Hydrochloride  |  Strontium Ranelate  |  Ligustroflavone  |  Calhex 231 hydrochloride  |  Calcium-Sensing Receptor Antagonists I  |  GSK3004774

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