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

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. 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].

In the type 1 diabetic model (T1D) rats, Calhex 231 (4.07 mg/kg; i.p.; daily; for 12 weeks; male Wistar rats) treatment ameliorates diabetic myocardial fibrosis [1].

2387505-78-2

C25H28Cl2N2O

443.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years