Calhex 231

Cat. No.: HY-103320: FAQs
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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).

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

Calhex 231 Chemical Structure

CAS No. : 652973-93-8

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Other In-stock Forms of Calhex 231:

Calhex 231 hydrochloride (1R,2R)-Calhex 231 hydrochloride

Other Forms of Calhex 231:

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

3 Publications Citing Use of MCE Calhex 231

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Description

IC₅₀ & Target

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

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^[2]

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

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^[2]
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

406.95

Formula

C₂₅H₂₇ClN₂O

CAS No.

652973-93-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Calhex 231 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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