Calhex 231
Based on 6 publication(s) in Google Scholar
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).
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- CAS No.: 652973-93-8
- Formule: C25H27ClN2O
- Masse moléculaire:406.95
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Stockage:
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Calhex 231
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Activité biologique
Calhex 231 dose-dependently inhibited the IP response induced by 10 mM Ca2+ with a potency in the T764A (IC50 = 0.28 ± 0.05 μM) and H766A (IC50 = 0.64 ± 0.03 μM) mutant receptors similar to that in the WT receptor[1].
Calhex 231 treatment significantly downregulates the CaSR, α-SMA, Col-I/III, MMP2/9 expresses. Calhex231 alleviates high glucose-induced myocardial fibrosis in cardiac fibroblasts[2].
Calhex 231 could inhibit Itch (atrophin-1 interacting protein 4)-ubiquitin proteasome and TGF-β1/Smads pathways, and then depress the proliferation of cardiac fibroblasts, along with the reduction deposition of collagen, alleviate glucose-induced myocardial fibrosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary neonatal rat cardiac fibroblasts (CFs).
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Concentration:3 µM.
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Incubation Time:24 hours.
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Result:Significantly decreased the proliferation of cardiac fibroblasts.
Calhex-231 (Cal, 0.1-1 mg/kg) has a mitigating effect on traumatic hemorrhagic shock by improving vascular hyporesponsiveness and reducing mitochondrial dysfunction[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (8 weeks old) injected with Streptozotocin[2]
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Dosage:4.07 mg/kg (10 µmoL/kg).
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Administration:Intraperitoneal injection; daily; for 12 weeks.
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Result:Ameliorated diabetic myocardial fibrosis in T1D rats.
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Animal Model:Four hundred and fifty Sprague-Dawley (SD) rats (half male and half female)[3].
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Dosage:0.1, 1, or 5 mg/kg.
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Administration:A continuous infusion.
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Result:In all groups, MAP, LVSP, and ±dp/dtmax decreased significantly after shock.
Administration of 5 or 1 mg/kg Cal resulted in significantly increased values at 1 and 2 hr postadministration, compared to rats in the LR only group (or 0.01).
Rats treated with 1 mg/kg Cal demonstrated the greatest recovery.
LR infusion induced short-term and slightly increase of blood pressor in normal rats.
Cal (1 mg/kg) without LR infusion did not restore the decreased MAP after shock.
Chemical Information
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CAS No. 652973-93-8
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Masse moléculaire 406.95
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Formule C25H27ClN2O
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Food Chem
Novel osteogenic peptide from bovine bone collagen hydrolysate: Targeted screening, molecular mechanism, and stability analysis. [Abstract]2024 Jul 6:459:140359. PMID: 38996641 -
Eur J Pharmacol
MFN2-dependent mitochondrial dysfunction contributes to Relm-β-induced pulmonary arterial hypertension via USP18/Twist1/miR-214 pathway. [Abstract]2024 Jul 31:980:176828. PMID: 39094924 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Mol Nutr Food Res
Novel Calcium-Binding Peptide from Bovine Bone Collagen Hydrolysates and Its Potential Pro-Osteogenic Activity via Calcium-Sensing Receptor (CaSR). [Abstract]2024 Feb;68(4):e2200726. PMID: 38161238 -
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J Nat Med
Nobiletin alleviates hypoxia-induced pulmonary hypertension by inhibiting calcium-sensing receptor. [Abstract]2025 Sep;79(5):1154-1166. PMID: 40581895
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Calhex 231 Related Classifications
HY-103320 Related Classifications
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