Calhex 231 hydrochloride

Cat. No. 4387

Calhex 231 hydrochloride C25H27ClN2O.HCl [652973-93-8]

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Chemical Name: 4-Chloro-N-[(1S,2S)-2-[[(1R)-1-(1-naphthalenyl)ethyl]amino]cyclohexyl]-benzamide hydrochloride

Biological Activity

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

M.Wt:
443.41
Formula:
C25H27ClN2O.HCl
Solubility:
Soluble to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
652973-93-8

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Weston et al (2008) The expression and function of Ca2+-sensing receptors in rat mesenteric artery; comparative studies using a model of type II diabetes. Br.J.Pharmacol. 154 652. PMID: 18414396.

Kessler et al (2006) 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. J.Med.Chem. 49 5119. PMID: 16913701.

Petrel et al (2003) Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca2+-sensing receptor. J.Biol.Chem. 278 49487. PMID: 14506236.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Calhex 231 hydrochloride include:

Yarova et al (2015) Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. Diabetologia 7 284ra60. PMID: 25904744.

Diakogiannaki et al (2013) Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor. Oncotarget 56 2688. PMID: 24045836.

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Keywords: Calhex 231 hydrochloride, supplier, Calhex231, calcilytics, hcasr, calcium-sensing, receptors, negative, allosteric, modulators, nams, Tocris Bioscience, Calcium-Sensing Receptor Modulator products

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