Catalog Number: 3626
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.
Technical Data
  • M.Wt:
    445.38
  • Formula:
    C24H25ClNO2.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    324523-20-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The search for calcium receptor antagonists (calcilytics).
    Nemeth
    J.Mol.Endocrinol., 2002;29:15
  2. 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
  3. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone.
    Nemeth et al.
    J.Pharmacol.Exp.Ther., 2001;299:323
Citations:

The citations listed below are publications that use Tocris products. Selected citations for NPS 2143 hydrochloride include:

5 Citations: Showing 1 - 5
Filter your results:

  1. Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
    Authors: Yarova Et al.
    Diabetologia 2015;7:284ra60
  2. Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension.
    Authors: Yamamura Et al.
    Sci Transl Med 2015;10:e0138384
  3. 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
  4. 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
  5. Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
    Authors: Yamamura Et al.
    Circ Res 2012;111:469

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