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2387505-78-2

中文名稱 Calhex 231 hydrochloride
英文名稱 Calhex 231 hydrochloride
CAS 2387505-78-2
分子式 C25H28Cl2N2O
分子量 443.41
MOL 文件 2387505-78-2.mol
2387505-78-2 結(jié)構(gòu)式 2387505-78-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10666

物理化學(xué)性質(zhì)

溶解度在DMSO中溶解至50mM
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Calhex 231 hydrochloride 是一種通過負(fù)變構(gòu)調(diào)節(jié)來抑制 CaSR 的。Calhex 231 hydrochloride 在 HEK293 細(xì)胞中阻斷 Ca2+ 誘導(dǎo)的肌醇磷酸酯的積累,IC50 為 0.39 μM。Calhex 231 hydrochloride 可用于糖尿病性心肌病 (DCM) 的研究。
靶點

CaSR
IC50: 0.39 μM (Inositol phosphate)

體外研究

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
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.
體內(nèi)研究

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.
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