Calhex 231 hydrochloride
Cat. No. 4387
Chemical Name: 4-Chloro-N-[(1S,2S)-2-[[(1R)-1-(1-n
Biological ActivityNegative 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).
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 Datasheet
References are publications that support the products' biological activity.
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.
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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.
Do you know of a great paper that uses Calhex 231 hydrochloride from Tocris? If so please let us know.
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