NPS 2143 hydrochloride
Chemical Name: 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino-2-hydroxypropoxy]benzonitrile hydrochloride
Purity: ≥99%
Biological Activity
NPS 2143 hydrochloride is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone.
Nemeth et al.
J.Pharmacol.Exp.Ther., 2001;299:323 -
The search for calcium receptor antagonists (calcilytics).
Nemeth
J.Mol.Endocrinol., 2002;29:15 -
Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis.
Huang and Breitwieser
J.Biol.Chem., 2007;282:9517
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Citations for NPS 2143 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for NPS 2143 hydrochloride include:
8 Citations: Showing 1 - 8
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Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine.
Authors: Zhang Et al.
Front Physiol 2019;9:1922
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Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
Authors: Yarova Et al.
Diabetologia 2015;7:284ra60
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Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension.
Authors: Yamamura Et al.
Sci Transl Med 2015;10:e0138384
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Calcium deficiency-induced and TRP channel-regulated IGF1R-PI3K-Akt signaling regulates abnormal epithelial cell proliferation.
Authors: Dai Et al.
Cell Death Differ 2014;21:568
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Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection.
Authors: Kim Et al.
Ann Clin Transl Neurol 2014;1:851
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Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor.
Authors: Diakogiannaki Et al.
Front Mol Neurosci 2013;56:2688
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Activation of the Ca2+-sensing receptor induces deposition of tight junction components to the epithelial cell plasma membrane.
Authors: Jouret Et al.
J Cell Sci 2013;126:5132
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Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
Authors: Yamamura Et al.
Circ Res 2012;111:469
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