Naftopidil dihydrochloride(Synonyms: KT-611 dihydrochloride; BM-15275 dihydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Naftopidil dihydrochloride (Synonyms: KT-611 dihydrochloride; BM-15275 dihydrochloride)

Naftopidil dihydrochloride (KT-611 dihydrochloride) 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 dihydrochloride 可用于前列腺增生的研究。

Naftopidil dihydrochloride(Synonyms: KT-611 dihydrochloride; BM-15275 dihydrochloride)

Naftopidil dihydrochloride Chemical Structure

CAS No. : 57149-08-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Naftopidil dihydrochloride 的其他形式现货产品:

Naftopidil

生物活性

Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b– and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia[1][2].

IC50 & Target[1]

Alpha-1A adrenergic receptor

3.7 nM (Ki)

Alpha-1B adrenergic receptor

20 nM (Ki)

Alpha-1D adrenergic receptor

1.2 (Ki)

体外研究
(In Vitro)

Naftopidil dihydrochloride suppresses human prostate tumor growth by altering interactions between tumor cells and stroma[2].
Naftopidil dihydrochloride (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC[2].
Naftopidil dihydrochloride (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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

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[2]

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
(In Vivo)

Naftopidil dihydrochloride (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic mice(7-8 weeks), with E9+PrSC xenograft[2]
Dosage: 10 mg/kg
Administration: Oral administration, daily, for 28 days
Result: Decreased tumor weights.

Clinical Trial

分子量

465.41

Formula

C24H30Cl2N2O3
CAS 号

57149-08-3
中文名称

萘哌地尔双盐酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R Takei, et al. Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol. 1999 Apr;79(4):447-54.

    [2]. Yasuhide Hori, et al. Naftopidil, a selective {alpha}1-adrenoceptor antagonist, suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Cancer Prev Res (Phila). 2011 Jan;4(1):87-96.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务