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/ Naftopidil

萘哌地尔 /Naftopidil {[allProObj[0].p_purity_real_show]}

货号：A109689 同义名： KT-611;BM-15275

Naftopidil是一种选择性的α1-肾上腺素受体拮抗剂（α阻滞剂），用于治疗良性前列腺增生（BPH）引起的下尿路症状（LUTS）。

Naftopidil 化学结构 CAS号：57149-07-2
Naftopidil 化学结构
CAS号：57149-07-2
Naftopidil 3D分子结构
CAS号：57149-07-2
Naftopidil 化学结构 CAS号：57149-07-2
Naftopidil 3D分子结构 CAS号：57149-07-2
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Naftopidil 纯度/质量文件 产品仅供科研

货号：A109689 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline hydrochloride ✔ 98%
Cisatracurium besylate ✔ 96%
Yohimbine HCI ✔ 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

 		+

β1-adrenoceptor, pIC50: 5.1

 		97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		99%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Doxazosin mesylate ✔ 99%
Tolazoline HCl ✔ 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Naftopidil 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].

Naftopidil 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 <<

Naftopidil 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.

Naftopidil 实验方案

计算器
存储液制备 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

Naftopidil 技术信息

CAS号57149-07-2
分子式C24H28N2O3
分子量 392.491
别名 KT-611;BM-15275;Flivas
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature
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

Tags: Naftopidil | 57149-07-2 | KT-611 | BM-15275 | KT611 | KT 611 | BM15275 | BM 15275 | Adrenergic Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Naftopidil 纯度/质量文件 | Naftopidil 亚型比较 | Naftopidil 生物活性 | Naftopidil 临床数据 | Naftopidil 参考文献 | Naftopidil 实验方案 | Naftopidil 技术信息

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