Calhex 231 hydrochloride
Chemical Name: 4-Chloro-N-[(1S,2S)-2-[[(1R)-1-(1-naphthalenyl)ethyl]amino]cyclohexyl]-benzamide hydrochloride
Purity: ≥98%
Biological Activity
Calhex 231 hydrochloride is a negative allosteric modulator of the calcium sensing receptor (CaSR). Blocks increases in [3H]inositol phosphate levels elicited by wild-type hCasR activation (IC50= 0.39 μM in transiently transfected HEK293 cells).Technical Data
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
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Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca2+-sensing receptor.
Petrel et al.
J.Biol.Chem., 2003;278:49487 -
The expression and function of Ca2+-sensing receptors in rat mesenteric artery; comparative studies using a model of type II diabetes.
Weston et al.
Br.J.Pharmacol., 2008;154:652 -
N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (Calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity.
Kessler et al.
J.Med.Chem., 2006;49:5119
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Citations for Calhex 231 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Calhex 231 hydrochloride include:
5 Citations: Showing 1 - 5
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Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation.
Authors: Ian P Et al.
Cell Signal 2023;107:110676
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Macrophages in obesity are characterised by increased IL-1β response to calcium-sensing receptor signals.
Authors: Ulf Et al.
Int J Obes (Lond) 2022;46:1883-1891
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Sensory Axon Growth Requires Spatiotemporal Integration of CaSR and TrkB Signaling.
Authors: Mathias Et al.
J Neurosci 2019;39:5842-5860
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Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
Authors: Yarova Et al.
Diabetologia 2015;7:284ra60
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Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor.
Authors: Diakogiannaki Et al.
Oncotarget 2013;56:2688
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