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盐酸萘哌地尔 /Naftopidil 2HCl {[allProObj[0].p_purity_real_show]}

货号:A127685 同义名: BM-15275 dihydrochloride;KT-611 dihydrochloride

Naftopidil 2HCl是一种选择性的 α1-肾上腺素受体拮抗剂,对 α1a、α1b 和 α1d 亚型的 Ki 值分别为 3.7 nM、20 nM 和 1.2 nM,主要用于治疗良性前列腺增生相关的下尿路症状。

Naftopidil 2HCl 化学结构 CAS号:57149-08-3
Naftopidil 2HCl 化学结构
CAS号:57149-08-3
Naftopidil 2HCl 3D分子结构
CAS号:57149-08-3
Naftopidil 2HCl 化学结构 CAS号:57149-08-3
Naftopidil 2HCl 3D分子结构 CAS号:57149-08-3
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Naftopidil 2HCl 纯度/质量文件 产品仅供科研

货号:A127685 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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Ivabradine HCl 98%
Maprotiline hydrochloride 98%
Cisatracurium besylate 96%
Yohimbine HCI 99+%
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

97%
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adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

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

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

99%
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Terazosin HCl 99%
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Phentolamine methanesulfonate salt 99%
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Zenidolol hydrochloride ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

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 2HCl 生物活性

靶点
  • α-adrenergic receptor

    α1-adrenergic receptor, IC50:0.2 μM

描述 Naftopidil (Dihydrochloride), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug. Naftopidil significantly improved the overall international prostatic symptom score[3]. The intravenous administration of each of Naftopidil dose-dependently inhibited phenylephrine-induced increases in prostatic pressure and mean blood pressure, the selectivity index was 3.76 [4]. Moreover, Naftopidil induces apoptosis and autophagy of HGC27 cells (human gastric cancer cell line), however, autophagy is considered to inhibit apoptosis[5].

Naftopidil 2HCl 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]Borbe HO, Metzenauer P, Szelenyi I. 5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug. Eur J Pharmacol. 1991 Nov 19;205(1):105-7.

[3]Sakai H, Igawa T, Onita T, Furukawa M, Hakariya T, Hayashi M, Matsuya F, Shida Y, Nishimura N, Yogi Y, Tsurusaki T, Takehara K, Nomata K, Shiraishi K, Shono T, Aoki D, Kanetake H. [Efficacy of naftopidil in patients with overactive bladder associated with benign prostatic hyperplasia: prospective randomized controlled study to compare differences in efficacy between morning and evening medication]. Hinyokika Kiyo. 2011 Jan;57(1):7-13. Japanese.

[4]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 Apr;79(4):447-54. doi: 10.1254/jjp.79.447. PMID: 10361884.

[5]Nakamura A, Matsunaga W, Gotoh A. Autophagy Induced by Naftopidil Inhibits Apoptosis of Human Gastric Cancer Cells. Anticancer Res. 2018 Feb;38(2):803-809.

Naftopidil 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.49mL

4.30mL

2.15mL

Naftopidil 2HCl 技术信息

CAS号57149-08-3
分子式C24H30Cl2N2O3
分子量 465.413
别名 BM-15275 dihydrochloride;KT-611 dihydrochloride;Naftopidil DiHCl;Naftopidil dihydrochloride
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
动物实验配方

0.5% CMC+water 30 mg/mL suspension

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