NPS 2143 hydrochloride

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Cat.No. 3626 - NPS 2143 hydrochloride | C24H25ClN2O2.HCl | CAS No. 324523-20-8
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)
Datasheet
Citations (8)
Reviews
Literature (1)

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.

Compound Libraries

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

M. Wt 445.38
Formula C24H25ClN2O2.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 324523-20-8
PubChem ID 9868131
InChI Key ZEBNDUQLNGYBNL-VEIFNGETSA-N
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

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

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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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8 Citations for NPS 2143 hydrochloride

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

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

Jouret et al (2013) Activation of the Ca2+-sensing receptor induces deposition of tight junction components to the epithelial cell plasma membrane. J Cell Sci 126 5132 PMID: 24013548

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

Zhang et al (2019) Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine. Front Physiol 9 1922 PMID: 30697165


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Literature in this Area

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