Calhex 231 (hydrochloride)

Calhex 231 hydrochloride 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 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) [1].

Product Specifications

CAS Number

[2387505-78-2]

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-hydrochloride.html

Purity

99.81

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

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.[H]Cl

Molecular Formula

C25H28Cl2N2O

Molecular Weight

443.41

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.