ChemicalBook CAS DataBase List 2387505-78-2

2387505-78-2

Name	Calhex 231 hydrochloride
CAS	2387505-78-2
Molecular Formula	C25H28Cl2N2O
MDL Number	MFCD22580412
Molecular Weight	443.41
MOL File	2387505-78-2.mol

Chemical Properties

solubility	Soluble to 50 mM in DMSO
form	Solid
color	White to off-white

Hazard Information

Biological Activity

Calhex 231 hydrochloride is a CaSR inhibitor through negative allosteric modulation. It blocks Ca2+-induced accumulation of inositol phosphate in HEK293 cells with IC50 of 0.39 μM. Calhex 231 hydrochloride can be used in the study of diabetic cardiomyopathy (DCM).

in vitro

Calhex 231 treatment significantly decreases the proliferation of cardiac fibroblasts.
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.
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.

Cell Proliferation Assay

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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

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. < /td>

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.

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

target

CaSR
IC50: 0.39 μM (Inositol phosphate)

storage

Store at -20°C

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

Shanghai EFE Biological Technology Co., Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

cjbscvictory

Telephone13348960310 13348960310

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Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 15801484223;

Websitehttp://www.jm-bio.com/

Bide Pharmatech Ltd.

Telephone400-1647117 13681763483

Websitehttps://www.bidepharm.com/

Kaifeng Mingren Pharmaceutical Co.,LTD

Telephone0371-65741762

Websitehttps://www.kfmryy.com/

TargetMol Chemicals Inc.

Telephone 4008200310

Websitehttps://www.targetmol.cn/

Nantong QuanYi Biotechnology Co., Ltd

Telephone0513-66337626 18051384581

Websitehttps://www.chemhifuture.com/

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