1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
- CAS号:1164469-60-6
- 英文名:1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
- 中文名:1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
- CBNumber:CB73845715
- 分子式:C24H29ClN2O3
- 分子量:428.95166
- MOL File:1164469-60-6.mol
- 储存条件 :Store at -20°C
- 溶解度 :DMF: 10 mg/mL; DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL; DMSO: 3 mg/mL
- 形态 :A crystalline solid
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride性质、用途与生产工艺
- 生物活性 Naftopidil hydrochloride (KT-611 hydrochloride) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力 Ki 值分别为 3.7 nM、20 nM、1.2 nM,具有抗增殖作用。Naftopidil hydrochloride 可用于前列腺增生的研究。
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靶点
Alpha-1A adrenergic receptor
3.7 nM (Ki)
Alpha-1B adrenergic receptor
20 nM (Ki)
Alpha-1D adrenergic receptor
1.2 nM (Ki)
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体外研究
Naftopidil hydrochloride suppresses human prostate tumor growth by altering interactions between tumor cells and stroma.
Naftopidil hydrochloride (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC.
Naftopidil hydrochloride (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.
Cell Proliferation Assay
Cell Line: PCa cells, PrSC Concentration: 10 μM (PCa cells); 0.1 μM, 1 μM, 10 μM (PrSC) Incubation Time: 3 days Result: Exhibited growth inhibitory effects on PCa cells and PrSC in dose-dependent manners. Western Blot Analysis
Cell Line: PCa cells, PrSC Concentration: 50 μM (E9 cells), 25 μM (PrSC) Incubation Time: 48 hours Result: Increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC. -
体内研究
Naftopidil hydrochloride (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model.
Animal Model: Male athymic mice(7-8 weeks), with E9+PrSC xenograft Dosage: 10 mg/kg Administration: Oral administration, daily, for 28 days Result: Decreased tumor weights.
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- 国家:英国
- 产品数:5729
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