Naftopidil

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Chemical Structure| 57149-07-2 同义名 : KT-611;BM-15275;Flivas
CAS号 : 57149-07-2
货号 : A109689
分子式 : C24H28N2O3
纯度 : 98%
分子量 : 392.491
MDL号 : MFCD00242741
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(89.17 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

生物活性
靶点

  • α-adrenergic receptor

    α1A-adrenergic receptor, Ki:3.7 nM

    α1D-adrenergic receptor, Ki:20 nM
描述 Naftopidil is a selective α1-adrenergic receptor antagonist or α receptor inhibitor with Ki of 58.3 nM. In vivo, forty minutes after the intravenous administration of naftopidil, the selectivity index was 3.76, naftopidil selectively inhibited the phenylephrine-induced increase in prostatic pressure[3]. In vitro, the concentrations causing 50% inhibition (IC50) of cancer cell growth were 22.2 ± 4.0 microM in androgen-sensitive LNCaP cells and 33.2 ± 1.1 microM in androgen-insensitive PC-3 cells. In vivo, oral administration of naftopidil to nude mice inhibited the growth of PC-3 tumors as compared to vehicle-treated controls[4]. Moreover, naftopidil induced apoptosis in all the investigated malignant mesothelioma cells[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01203371 Hyperplasia Phase 3 Unknown January 2012 Brazil ... 展开 >> Hospital das Clínicas da Faculdade de Medicina da USP Not yet recruiting São Paulo, Brazil, 05403-010 Contact: Geraldo C Freire, PhD    55 11 3069-8082       Contact: Camila C Marin    55 11 3069-8082    camila.marin@ig.com.br    Principal Investigator: Geraldo C Freire, PhD 收起 <<
NCT02034604 Neurogenic Lower Urinary Tract... 展开 >> Dysfunction 收起 << Phase 4 Unknown April 2015 Korea, Republic of ... 展开 >> Samsung Medical Center Recruiting Seoul, Korea, Republic of, 130-710 Contact: Kyu-Sung Lee, M.D., Ph.D.    82-2-3410-3554    ksleedr@skku.edu    Contact: Hyun Wook You, M.D.    82-2-3410-1268    khdoct29@gmail.com    Principal Investigator: Kyu-Sung Lee, Ph.D, M.D. 收起 <<
NCT01922375 Lower Urinary Tract Symptoms A... 展开 >>ssociated With Benign Prostatic Hyperplasia 收起 << Phase 4 Completed - Korea, Republic of ... 展开 >> Chonnam national university hospital Gwangju, Korea, Republic of 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL
参考文献

[1]Kanda H, Ishii K, et al. Naftopidil, a selective alpha-1 adrenoceptor antagonist, inhibits growth of human prostate cancer cells by G1 cell cycle arrest. Int J Cancer. 2008 Jan 15;122(2):444-51.

[2]Takei R, Ikegaki I, 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.

[3]Takei R, Ikegaki I, Shibata K, Tsujimoto G, Asano T. 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;79(4):447-454.

[4]Kanda H, Ishii K, Ogura Y, et al. Naftopidil, a selective alpha-1 adrenoceptor antagonist, inhibits growth of human prostate cancer cells by G1 cell cycle arrest. Int J Cancer. 2008;122(2):444-451.

[5]Masachika E, Kanno T, Nakano T, Gotoh A, Nishizaki T. Naftopidil induces apoptosis in malignant mesothelioma cell lines independently of α1-adrenoceptor blocking. Anticancer Res. 2013;33(3):887-894.