1. GPCR/G Protein
  2. CaSR
  3. Calhex 231 hydrochloride

Calhex 231 hydrochloride 

Cat. No.: HY-103320A Purity: >98.0%
Handling Instructions

Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca2+-induced accumulation of [3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.

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Calhex 231 hydrochloride Chemical Structure

Calhex 231 hydrochloride Chemical Structure

CAS No. : 2387505-78-2

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Description

Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca2+-induced accumulation of [3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment[1][2].

IC50 & Target

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

In Vitro

Calhex 231 treatment significantly decreases the proliferation of cardiac fibroblasts[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[1].
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[1].

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[1].

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.
Molecular Weight

443.41

Formula

C₂₅H₂₈Cl₂N₂O

CAS No.

2387505-78-2

SMILES

O=C(N[[email protected]@H]1[[email protected]@H](N[[email protected]@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
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

Calhex 231Calhex231Calhex-231CaSRCalcium-sensing receptorDiabeticcardiomyopathyfibrosisG-proteinα-SMATGF-β1ItchcollagennegativeallostericinositolInhibitorinhibitorinhibit

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Calhex 231 hydrochloride
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