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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 | Cell Line: | Primary neonatal rat cardiac fibroblasts (CFs) | | Concentration: | 3 μM | td> | 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 |
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