Calhex 231 hydrochloride
- CAS No.
- 2387505-78-2
- Chemical Name:
- Calhex 231 hydrochloride
- Synonyms
- CBNumber:
- CB48054344
- Molecular Formula:
- C25H28Cl2N2O
- Molecular Weight:
- 443.41
- MDL Number:
- MFCD22580412
- MOL File:
- 2387505-78-2.mol
Calhex 231 hydrochloride Chemical Properties,Uses,Production
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
| 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
Calhex 231 hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
Calhex 231 hydrochloride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3421 | 58 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9709 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 9946 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223 | psaitong@jm-bio.com | China | 29834 | 58 |
| Kaifeng Mingren Pharmaceutical Co.,LTD | 0371-65741762 | sales@hasunny.com | China | 2380 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4030 | 58 |