NPS 2143 hydrochlorideCat. No. 3626 |
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Chemical Name: 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino-2-hydroxypropoxy]benzonitrile hydrochloride |
Biological Activity
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.Certificate of Analysis / Safety Data Sheet
References
Nemeth et al (2001) Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J.Pharmacol.Exp.Ther. 299 323. PMID: 11561095.
Nemeth (2002) The search for calcium receptor antagonists (calcilytics). J.Mol.Endocrinol. 29 15. PMID: 12200226.
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. PMID: 17284438.
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Keywords: NPS 2143 hydrochloride, supplier, calcium, Ca2+, sensing, receptors, CaSR, antagonists, orally, active, calcilytics, NPS2143
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