Calhex 231 hydrochloride

Name: Calhex 231 hydrochloride
Brand: MedChemExpress
SKU: HY-103320A
Rating: 4.5 (3 reviews)

Cat. No.: HY-103320A Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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).

For research use only. We do not sell to patients.

Calhex 231 hydrochloride Chemical Structure

CAS No. : 2387505-78-2

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Calhex 231 hydrochloride:

(1R,2R)-Calhex 231 hydrochloride In-stock
Calhex 231 Get quote

3 Publications Citing Use of MCE Calhex 231 hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CaSR^[1]
IC50: 0.39 μM (Inositol phosphate)^[2]

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.

Cell Proliferation Assay^[1]

Cell Line:	Primary neonatal rat cardiac fibroblasts (CFs)
Concentration:	3 µM
Incubation Time:	24 hours
Result:	Significantly decreased the proliferation of cardiac fibroblasts.

Western Blot Analysis^[1]

Cell Line:	Primary neonatal rat cardiac fibroblasts (CFs)
Concentration:	3 µM
Incubation Time:	48 hours
Result:	The expression of CaSR, α-SMA, Col-I/III, MMP2/9 were significantly downregulated.

In Vivo

Calhex 231 (4.07 mg/kg (10 µmol/kg); intraperitoneal injection; daily; for 12 weeks; male Wistar rats) treatment ameliorates diabetic myocardial fibrosis in type 1 diabetic model (T1D) rats^[2].
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.

Animal Model:	Male Wistar rats (8 weeks old) injected with Streptozotocin^[1]
Dosage:	4.07 mg/kg (10 µmol/kg)
Administration:	Intraperitoneal injection; daily; for 12 weeks
Result:	Ameliorated diabetic myocardial fibrosis in T1D rats.

Animal Model:	Four hundred and fifty Sprague-Dawley (SD) rats (half male and half female)^[3].
Dosage:	0.1, 1, or 5 mg/kg.
Administration:	A continuous infusion.
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.

Molecular Weight

443.41

Formula

C₂₅H₂₈Cl₂N₂O

CAS No.

2387505-78-2

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2552 mL	11.2762 mL	22.5525 mL
5 mM	0.4510 mL	2.2552 mL	4.5105 mL
10 mM	0.2255 mL	1.1276 mL	2.2552 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (281 KB) SDS (251 KB)

COA (251 KB) LCMS (304 KB)

Handling Instructions (2659 KB)

References

[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

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