NPS 2143 hydrochloride

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Cat.No. 3626 - NPS 2143 hydrochloride | C24H25ClN2O2.HCl | CAS No. 324523-20-8
Description: Selective antagonist of the calcium-sensing receptor; 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 (6)
Reviews
Literature

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

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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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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Safety Datasheet

References

References are publications that support the products' biological activity.

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

6 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

Kim et al (2014) Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection. Ann Clin Transl Neurol 1 851 PMID: 25540800

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


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