Calhex 231

• Description:

  Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) [1].

• UNSPSC:

  12352005

• Target:

  CaSR

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  Metabolism-sugar/lipid metabolism

• Field of Research:

  Metabolic Disease

• Assay Protocol:

  https://www.medchemexpress.com/calhex-231.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(N[C@@H]1[C@@H](N[C@@H](C2=C3C=CC=CC3=CC=C2)C)CCCC1)C4=CC=C(Cl)C=C4

• Molecular Formula:

  C25H27ClN2O

• Molecular Weight:

  406.95

• References & Citations:

  [1]Christophe Petrel, et al. Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca (2+) -sensing receptor. J Biol Chem. 2003 Dec 5;278 (49) :49487-94.|[2]Petrel C1, et al. Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca (2+) -sensing receptor. J Biol Chem. 2003 Dec 5;278 (49) :49487-94.|[3]Yan Lei, et al. The Calcilytic Drug Calhex-231 Ameliorates Vascular Hyporesponsiveness in Traumatic Hemorrhagic Shock by Inhibiting Oxidative Stress and miR-208a-Mediated Mitochondrial Fission. Oxid Med Cell Longev. 2020 Dec 3:2020:4132785.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Citation 01:

  Eur J Pharmacol. 2024 Jul 31:980:176828.|J Nat Med. 2025 Sep;79 (5) :1154-1166.|Food Chem. 2024 Jul 6:459:140359.|Front Pharmacol. 2022 Feb 23:13:816133.|Front Pharmacol. 2022 Feb 23;13:816133.|J Funct Foods. 2025 Apr.|Mol Nutr Food Res. 2024 Feb;68 (4) :e2200726.

• CAS Number:

  652973-93-8