NPS 2143 hydrochloride
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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
7 Citations for NPS 2143 hydrochloride
Citations are publications that use Tocris products. Selected citations for NPS 2143 hydrochloride include:
Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469 PMID: 22730443
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
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
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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