Calhex 231 hydrochloride
Based on 6 publication(s) in Google Scholar
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).
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- Pureté : 99.36%
- CAS No.: 2387505-78-2
- Formule: C25H28Cl2N2O
- Masse moléculaire:443.41
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Calhex 231 hydrochloride
More
Activité biologique
Description
IC50 & Target
In Vitro
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.
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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:48 hours
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Result:The expression of CaSR, α-SMA, Col-I/III, MMP2/9 were significantly downregulated.
In Vivo
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[1]
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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. 2387505-78-2
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Appearance Solid
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Masse moléculaire 443.41
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Formule C25H28Cl2N2O
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Color White to off-white
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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.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 Nov 30:459:140359. 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 Oct 5:980:176828. 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
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (75.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2552 mL | 11.2762 mL | 22.5525 mL | 56.3812 mL |
| 5 mM | 0.4510 mL | 2.2552 mL | 4.5105 mL | 11.2762 mL | |
| 10 mM | 0.2255 mL | 1.1276 mL | 2.2552 mL | 5.6381 mL | |
| 15 mM | 0.1503 mL | 0.7517 mL | 1.5035 mL | 3.7587 mL | |
| 20 mM | 0.1128 mL | 0.5638 mL | 1.1276 mL | 2.8191 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9021 mL | 2.2552 mL | |
| 30 mM | 0.0752 mL | 0.3759 mL | 0.7517 mL | 1.8794 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5638 mL | 1.4095 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1276 mL | |
| 60 mM | 0.0376 mL | 0.1879 mL | 0.3759 mL | 0.9397 mL |
Calhex 231 hydrochloride Related Classifications
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