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Calhex 231 hydrochloride

Cat. No. 4387

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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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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.

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.

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