NPS 2143 hydrochloride
Chemical Name: 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino-2-hydroxypropoxy]benzonitrile hydrochloride
Biological ActivitySelective 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone.
Nemeth et al.
The search for calcium receptor antagonists (calcilytics).
Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis.
Huang and Breitwieser
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
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
Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
Authors: Yarova Et al.
Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension.
Authors: Yamamura Et al.
Sci Transl Med 2015;10:e0138384
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
Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection.
Authors: Kim Et al.
Ann Clin Transl Neurol 2014;1:851
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
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
Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
Authors: Yamamura Et al.
Circ Res 2012;111:469
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