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Submit ReviewNPS 2143 hydrochloride
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)
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 |
| 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 for NPS 2143 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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
If you know of a relevant reference for NPS 2143 hydrochloride, please let us know.
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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:
Bidhan C et al (2020) l-ornithine activates Ca2+ signaling to exert its protective function on human proximal tubular cells. Cell Signal 67 109484 PMID: 31770578
Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469 PMID: 22730443
Ian P et al (2023) Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation. Cell Signal 107 110676 PMID: 37028778
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
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
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
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
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
Donald T et al (2021) Study of the Expression and Function of Calcium-Sensing Receptor in Human Skeletal Muscle. Int J Mol Sci 22 PMID: 34298895
Catherine A et al (2022) Calcium-sensing receptor and CPAP-induced neonatal airway hyperreactivity in mice. Pediatr Res 91 1391-1398 PMID: 33958714
Silvia F et al (2022) Regulation of Stanniocalcin Secretion by Calcium and PTHrP in Gilthead Seabream (Sparus aurata). Biology (Basel) 11 PMID: 35741384
Kim et al (2014) Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection. Ann Clin Transl Neurol 1 851 PMID: 25540800
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