Calhex 231
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].
Product Specifications
CAS Number
652973-93-8
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.
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