284035-33-2

溶解度:Desiccate at RT

储存条件:at -20℃ 2 years

生物活性

Selective Ca2+-sensing receptor antagonist. Blocks increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells (IC50 = 43 nM). Also stimulates parathyroid hormone secretion from bovine parathyroid cells (EC50 = 41 nM). Orally active calcilytic compound.

参考文献

Nemeth et al (2001) Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J.Pharmacol.Exp.Ther. 299 323. Nemeth (2002) The search for calcium receptor antagonists (calcilytics). J.Mol.Endocrinol. 29 15. Huang and Breitwieser (2007) Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J.Biol.Chem. 282 9517.