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NPS 2143 hydrochloride

Catalog #: 3626
13 Citations Datasheet / COA / SDS
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3626/50
NPS 2143 hydrochloride | CAS No. 324523-20-8 | Calcium-Sensing Receptor Antagonists
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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%

Product Details
Citations (13)
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Biological Activity

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.

Technical Data

M.Wt:
445.38
Formula:
C24H25ClN2O2.HCl
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
324523-20-8

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.

Background References

  1. Extracellular Ca(2+) sensing in salivary ductal cells.
    Bandyopadhyay, Bidhan C, Swaim, William, Sarkar, Ankana, Liu, Xibao, Ambudkar, Indu S
    J Biol Chem, 2012;287(36):30305-16.
  2. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone.
    Nemeth et al.
    J.Pharmacol.Exp.Ther., 2001;299:323
  3. The search for calcium receptor antagonists (calcilytics).
    Nemeth
    J.Mol.Endocrinol., 2002;29:15
  4. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis.
    Huang and Breitwieser
    J.Biol.Chem., 2007;282:9517

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Citations for NPS 2143 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for NPS 2143 hydrochloride include:

13 Citations: Showing 1 - 10

  1. Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation.
    Authors: Ian P Et al.
    Cell Signal  2023;107:110676
  2. Calcium-sensing receptor and CPAP-induced neonatal airway hyperreactivity in mice.
    Authors: Catherine A Et al.
    Pediatr Res  2022;91:1391-1398
  3. Regulation of Stanniocalcin Secretion by Calcium and PTHrP in Gilthead Seabream (Sparus aurata).
    Authors: Silvia F Et al.
    Biology (Basel)  2022;11
  4. Study of the Expression and Function of Calcium-Sensing Receptor in Human Skeletal Muscle.
    Authors: Donald T Et al.
    Int J Mol Sci  2021;22
  5. l-ornithine activates Ca2+ signaling to exert its protective function on human proximal tubular cells.
    Authors: Bidhan C Et al.
    Cell Signal  2020;67:109484
  6. Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine.
    Authors: Zhang Et al.
    Front Physiol  2019;9:1922
  7. Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
    Authors: Yarova Et al.
    Diabetologia  2015;7:284ra60
  8. Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension.
    Authors: Yamamura Et al.
    Sci Transl Med  2015;10:e0138384
  9. Calcium deficiency-induced and TRP channel-regulated IGF1R-PI3K-Akt signaling regulates abnormal epithelial cell proliferation.
    Authors: Dai Et al.
    Cell Death Differ  2014;21:568
  10. Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection.
    Authors: Kim Et al.
    Ann Clin Transl Neurol  2014;1:851

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