1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
| 中文名称 | 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride |
|---|---|
| 中文同义词 | 萘哌地尔盐酸盐;NAFTOPIDIL HYDROCHLORIDE,Α1拮抗剂 |
| 英文名称 | 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride |
| 英文同义词 | 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride;BM-15275 hydrochloride;KT-611 hydrochloride;BM-15275,BM15275,canine,prostatic,Naftopidil,prostate,hyperplasia,inhibit,Inhibitor,Naftopidil hydrochloride,KT-611,Adrenergic Receptor,KT611,KT 611,pressure,BM 15275,Beta Receptor;Emorfazone Impurity 3 |
| CAS号 | 1164469-60-6 |
| 分子式 | C24H29ClN2O3 |
| 分子量 | 428.95166 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1164469-60-6.mol |
| 结构式 | ![1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride 结构式](CAS/20180601/GIF/1164469-60-6.gif) |
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride 性质
| 储存条件 | Store at -20°C |
|---|---|
| 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 |
|
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. |