NPS 2143 hydrochloride

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Description: Selective calcium-sensing receptor (CaSR) antagonist; orally active calcilytic agent
Chemical Name: 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino-2-hydroxypropoxy]benzonitrile hydrochloride
Purity: ≥99% (HPLC)
Citations (13)

Biological Activity for NPS 2143 hydrochloride

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.

Compound Libraries for NPS 2143 hydrochloride

NPS 2143 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for NPS 2143 hydrochloride

M. Wt 445.38
Formula C24H25ClN2O2.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 324523-20-8
PubChem ID 9868131
Smiles CC(NC[C@@H](O)COC3=C(C#N)C(Cl)=CC=C3)(C)CC2=CC1=CC=CC=C1C=C2.Cl

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.

Solubility Data for NPS 2143 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 44.54 100
ethanol 4.45 10

Preparing Stock Solutions for NPS 2143 hydrochloride

The following data is based on the product molecular weight 445.38. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.25 mL 11.23 mL 22.45 mL
5 mM 0.45 mL 2.25 mL 4.49 mL
10 mM 0.22 mL 1.12 mL 2.25 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets for NPS 2143 hydrochloride

Certificate of Analysis / Product Datasheet
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References for NPS 2143 hydrochloride

References are publications that support the biological activity of the product.

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, NPS 2143 hydrochloride supplier, calcium, Ca2+, sensing, receptors, CaSR, antagonists, orally, active, calcilytics, NPS2143, Calcium-Sensing, Receptor, 3626, Tocris Bioscience

13 Citations for NPS 2143 hydrochloride

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

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

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

Do you know of a great paper that uses NPS 2143 hydrochloride from Tocris? Please let us know.

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