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Chemical Structure| 2387505-78-2 Chemical Structure| 2387505-78-2

Structure of Calhex 231 HCl
CAS No.: 2387505-78-2

Chemical Structure| 2387505-78-2

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Calhex 231 hydrochloride is a compound that inhibits the calcium-sensing receptor (CaSR) through negative allosteric modulation, blocking Ca2+-induced inositol phosphate accumulation, with an IC50 of 0.39 μM. This compound is widely used in research on diabetic cardiomyopathy (DCM) and other calcium regulation-related diseases.

Synonyms: Calhex 231 hydrochloride

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Product Details of Calhex 231 HCl

CAS No. :2387505-78-2
Formula : C25H28Cl2N2O
M.W : 443.41
SMILES Code : O=C(C1=CC=C(C=C1)Cl)N[C@@H]2[C@H](CCCC2)N[C@H](C)C3=C4C=CC=CC4=CC=C3.[H]Cl
Synonyms :
Calhex 231 hydrochloride
MDL No. :MFCD22580412

Safety of Calhex 231 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Calhex 231 HCl

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
rabbit mesenteric artery smooth muscle cells 1 µM, 3 µM, 10 µM inhibited whole-cell VGCC currents by approximately 25%, 60%, and 95% respectively Eur J Pharmacol. 2016 Nov 15;791:659-668
rabbit mesenteric artery endothelial cells (ECs) 3 μM 20 min To investigate the inhibitory effect of Calhex-231 on CaSR-mediated NO production, results showed that Calhex-231 inhibited [Ca2+]o-induced NO production. Vascul Pharmacol. 2016 May;80:75-84
rabbit mesenteric artery endothelial cells (ECs) 3 μM 30 min To investigate the inhibitory effect of Calhex-231 on CaSR-mediated vasorelaxation, results showed that Calhex-231 significantly inhibited [Ca2+]o-induced vasorelaxation. Vascul Pharmacol. 2016 May;80:75-84
mouse descending colon mucosa 10 μM inhibited Gln-induced changes in Isc Br J Pharmacol. 2013 Nov;170(5):1092-101
HepG2 cells 10 µM 120 h Inhibits CaSR activation, preventing HepG2 cell senescence and mitochondrial dysfunction Int J Mol Sci. 2023 Mar 9;24(6):5217
SW872 pre-adipocytes 10 µM 16 h Inhibits calcium-sensing receptor (CaSR) activation, preventing pro-inflammatory factor secretion from pre-adipocytes Int J Mol Sci. 2023 Mar 9;24(6):5217
rat mesenteric artery endothelial cells 1 μM and 3 μM Calhex 231 inhibited calindol-induced myocyte hyperpolarization, indicating its role as a negative allosteric modulator of CaR. Br J Pharmacol. 2008 Jun;154(3):652-62

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice PYY knockout mice 10 μM Inhibited Gln-induced changes in Isc Br J Pharmacol. 2013 Nov;170(5):1092-101

Protocol

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11.28mL

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1.13mL

22.55mL

4.51mL

2.26mL

 

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