NPS-2143 hydrochloride
| CAS号 | 324523-20-8 | 货号 | BCP16483 |
| 中文名 | NPS-2143 hydrochloride | ||
| 英文名 | NPS-2143 hydrochloride | ||
| 中文别名 | |||
| 英文别名 | NPS 2143 hydrochloride;NPS2143 hydrochloride,SB 262470 HCl; | ||
| 分子式 | C24H26Cl2N2O2 | 分子量 | 445.38 |
| 生物活性 | IC50 value: 43 nM(for Ca2+ receptor) Target: CaSR in vitro: NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH. The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH . in vivo: When infused intravenously in normal rats, NPS 2143 caused 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 agen | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | CaSR | ||
结构式
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