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1164469-60-6

中文名稱 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
英文名稱 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
CAS 1164469-60-6
分子式 C24H29ClN2O3
分子量 428.952
MOL 文件 1164469-60-6.mol
1164469-60-6 結構式 1164469-60-6 結構式

基本信息

中文別名
萘哌地爾鹽酸鹽
英文別名
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride

物理化學性質

儲存條件-20°C儲存
溶解度DMF: 10 mg/mL; DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL; DMSO: 3 mg/mL
形態(tài)結晶固體

常見問題列表

生物活性
Naftopidil hydrochloride (KT-611 hydrochloride) 是一種選擇性的 alpha1-腎上腺素受體 (α1-adrenoceptor) 拮抗劑,對克隆的人類 α1a、α1b 和 α1d 亞型腎上腺素受體的親和力 Ki 值分別為 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。
靶點

Alpha-1A adrenergic receptor

3.7 nM (Ki)

Alpha-1B adrenergic receptor

20 nM (Ki)

Alpha-1D adrenergic receptor

1.2 nM (Ki)

體外研究

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.
體內研究

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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