| 货号 | 17903-1mg |
| 描述 | Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.1,2 Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.1,2 NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro(EC50 = 39 nM).3,4 It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.3,4 Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.3 |
| 别名 | SB-262470A; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Nemeth, E.F. The search for calcium receptor antagonists (calcilytics). Journal of Molecular Endocrinology 29, 15-21 (2002). 2.Filopanti, M.,Corbetta, S.,Barbieri, A.M., et al. Pharmacology of the calcium sensing receptor. Clin.Cases Miner.Bone Metab. 10(3), 162-165 (2013). 3.Gowen, M.,Stroup, G.B.,Dodds, R.A., et al. Antagonizing the parathyroid calcium receptor stimulates parathyroid hormone secretion and bone formation in osteopenic rats. Journal of Clinical Investigation 105, 1595-1604 (2000). 4.Nemeth, E.F.,DelMar, E.G.,Heaton, W.L., et al. Calcilytic compounds: Potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. JPET 299(1), 323-331 (2001). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 445.4 |
| 分子式 | C24H25ClN2O2 • HCl |
| CAS号 | 324523-20-8 |
| 稳定性 | ≥ 2 years |
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