1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride 性质
储存条件 | Store at -20°C |
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溶解度 | DMF:10mg/mL; DMF:PBS (pH 7.2) (1:4):0.2 mg/mL;二甲基亚砜:3mg/mL |
形态 | 结晶固体 |
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride 用途与合成方法
Alpha-1A adrenergic receptor 3.7 nM (Ki) |
Alpha-1B adrenergic receptor 20 nM (Ki) |
Alpha-1D adrenergic receptor 1.2 nM (Ki) |
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. |
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. |