Calhex 231 hydrochloride  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(33.33mg/mL 超声)
产品描述:基本信息 产品编号: C110990 产品名称: Calhex 231 hydrochloride CAS: 2387505-78-2   储存条件 粉末 -20℃ 四年 分子式: C25H28Cl2N2O 溶于液体 -80℃ 6个月 分子量: 443.41 -20℃ 1个月 化学名:  4-chloro-N-[(1S,2S)-2-[[(1R)-1-naphthalen-1-ylethyl]amino]cyclohexyl]benzamide;hydrochloride Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.2552mL 11.2762mL 22.5525mL 5mM 0.4510mL 2.2552mL 4.5105mL 10mM 0.2255mL 1.1276mL 2.2552mL   生物活性 产品描述 一种通过负变构调节来抑制 CaSR的。Calhex 231 hydrochloride 在 HEK293 细胞中阻断 Ca2+诱导的肌醇磷酸酯的积累,IC50为0.39μM。Calhex 231 hydrochloride 可用于糖尿病性心肌病 (DCM) 的研究。 靶点 CaSR IC50:0.39μM (Inositol phosphate)   体外研究 Calhex231 treatment significantly decreases the proliferation of cardiac fibroblasts.Calhex231 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: 3µM Incubation Time: 24 hours Result: Significantly decreased the proliferation of cardiac fibroblasts. Western Blot Analysis Cell Line: Primary neonatal rat cardiac fibroblasts (CFs) Concentration: 3µM Incubation Time: 48 hours Result: The expression of CaSR,α-SMA,Col-I/III,MMP2/9 were significantly downregulated. 体内研究 Calhex 231 (4.07mg/kg (10µmol/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: 4.07mg/kg (10µmol/kg) Administration: Intraperitoneal injection;daily;for 12 weeks Result: Ameliorated diabetic myocardial fibrosis in T1D rats.
保存条件:-20℃