NPS 2143 hydrochloride

Cat. No. 3626

NPS 2143 hydrochloride C24H25ClNO2.HCl [324523-20-8]

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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.

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

Nemeth (2002) The search for calcium receptor antagonists (calcilytics). J.Mol.Endocrinol. 29 15. PMID: 12200226.

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.

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Citations are publications that use Tocris products. Selected citations for NPS 2143 hydrochloride include:

Yamamura et al (2015) Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension. Sci Transl Med 10 e0138384. PMID: 26375676.

Yarova et al (2015) Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. Diabetologia 7 284ra60. PMID: 25904744.

Dai et al (2014) Calcium deficiency-induced and TRP channel-regulated IGF1R-PI3K-Akt signaling regulates abnormal epithelial cell proliferation. Cell Death Differ 21 568. PMID: 24336047.

Diakogiannaki et al (2013) Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor. Front Mol Neurosci 56 2688. PMID: 24045836.

Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469. PMID: 22730443.

Do you know of a great paper that uses NPS 2143 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: NPS 2143 hydrochloride, supplier, calcium, Ca2+, sensing, receptors, CaSR, antagonists, orally, active, calcilytics, NPS2143, Tocris Bioscience, Calcium-Sensing Receptor Antagonist products

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