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盐酸阿夫唑嗪 /Alfuzosin HCl {[allProObj[0].p_purity_real_show]}

货号:A272742 同义名: 阿夫唑嗪盐酸盐 / SL 77499-10;Alfuzosin (hydrochloride)

Alfuzosin HCl is an antagonist of α1 adrenergic receptor used to treat benign prostatic hyperplasia (BPH).

Alfuzosin HCl 化学结构 CAS号:81403-68-1
Alfuzosin HCl 化学结构
CAS号:81403-68-1
Alfuzosin HCl 3D分子结构
CAS号:81403-68-1
Alfuzosin HCl 化学结构 CAS号:81403-68-1
Alfuzosin HCl 3D分子结构 CAS号:81403-68-1
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Alfuzosin HCl 纯度/质量文件 产品仅供科研

货号:A272742 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 98%
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 +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
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。

Alfuzosin HCl 生物活性

靶点
  • α-adrenergic receptor

描述 Alfuzosin hydrochloride is a selective and competitive α1-adrenoceptor antagonist for the treatment of symptomatic BPH (benign prostatic hyperplasia)[3]. In the pithed rat, alfuzosin (0.03-0.3 mg kg-1, i.v.) markedly inhibited pressor responses produced by the alpha 1-selective agonist; alfuzosin (1 mg kg-1, i.v.) had minimal effects against responses mediated by stimulation of prejunctional alpha 2-receptors[4]. Moreover, Alfuzosin hydrochloride is an appropriate candidate drug to prepare a gastro-retention controlled release dosage form[5].

Alfuzosin HCl 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
NCT01685658 Renal Colic A... 展开 >>cute Renal Colic 收起 << Phase 4 Suspended(same study already p... 展开 >>ublished) 收起 << March 2018 France ... 展开 >> CH d'Alès Alès, France, 30103 CHU de Nîmes - Hôpital Universitaire Carémeau Nîmes Cedex 9, France, 30029 收起 <<
NCT01323998 - Completed - -
NCT01332487 - Completed - -

Alfuzosin HCl 参考文献

[1]Lacerda AE, Kuryshev YA, et al. Alfuzosin delays cardiac repolarization by a novel mechanism. J Pharmacol Exp Ther. 2008 Feb;324(2):427-33.

[2]Palea S, Barras M. Comparison of the relaxant effects of alfuzosin, phentolamine and sildenafil on rabbit isolated corpus cavernosum. BJU Int. 2003 Jun;91(9):873-7.

[3]Fahmy RH. Statistical approach for assessing the influence of calcium silicate and HPMC on the formulation of novel alfuzosin hydrochloride mucoadhesive-floating beads as gastroretentive drug delivery systems. AAPS PharmSciTech. 2012 Sep;13(3):990-1004.

[4]Lefèvre-Borg F, O'Connor SE, Schoemaker H, Hicks PE, Lechaire J, Gautier E, Pierre F, Pimoule C, Manoury P, Langer SZ. Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol. 1993 Aug;109(4):1282-9.

[5]Gong L, Sun Y, Yu M, Gao Y, Zou M, Cheng G. Development and Evaluation of Compression Coating Gastro-Floating Tablet of Alfuzosin Hydrochloride for Zero-Order Controlled Release. AAPS PharmSciTech. 2018 Oct;19(7):3277-3286.

Alfuzosin HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.74mL

2.35mL

1.17mL

23.48mL

4.70mL

2.35mL

Alfuzosin HCl 技术信息

CAS号81403-68-1
分子式C19H28ClN5O4
分子量 425.91
别名 阿夫唑嗪盐酸盐 ;SL 77499-10;Alfuzosin (hydrochloride);Uroxatral;SL 77499 HCl;Alfuzosin HCl
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 25 mg/mL(58.7 mM),配合低频超声,并水浴加热至45℃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

H2O: 50 mg/mL(117.4 mM),配合低频超声助溶

动物实验配方
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