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

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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

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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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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.

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