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普罗地芬 盐酸盐 /Proadifen HCl {[allProObj[0].p_purity_real_show]}

货号:A263311 同义名: 盐酸丙基解痉素 / SKF-525A;U-5446

Proadifen HCl是一种非特异性的细胞色素P450抑制剂,还是乙酰胆碱尼古丁受体的非竞争性抑制剂,IC50值为19 μM,在小鼠骨骼肌中表现抑制作用。

Proadifen HCl 化学结构 CAS号:62-68-0
Proadifen HCl 化学结构
CAS号:62-68-0
Proadifen HCl 3D分子结构
CAS号:62-68-0
Proadifen HCl 化学结构 CAS号:62-68-0
Proadifen HCl 3D分子结构 CAS号:62-68-0
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Proadifen HCl 纯度/质量文件 产品仅供科研

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Proadifen HCl 生物活性

描述 Proadifen (SKF-525A) HCl is a P450 monooxygenase inhibitor with potential anti-proliferative activity and the ability to potentiate the toxicity of hypericin-mediated photodynamic therapy and mitoxantrone via alteration of ABC transport proteins[2]. Adult male Wistar rats were administered SKF525 (proadifen hydrochloride) forty-eight, twenty-four, and one hour before electrophysiological assessments. It was found that the SKF525 inhibits the excitability of 5-HT neurons[3]. Proadifen inhibited the growth of HT-29 cells by the accumulation of cells in the G1 phase of the cell cycle, reduction of metabolic activity and colony formation and by the induction of apoptosis[4]. Moreover, proadifen (10 mM) also inhibited acetylcholine-induced hyperpolarization in the presence of L-NOARG plus indomethacin[5]. Proadifen may possess complex interactions with muscarinic receptors and Ca2+ entry blocking properties in concentrations 10-100 times lower than those reported to inhibit cytochrome P450-catalysed reactions[6].

Proadifen HCl 参考文献

[1]Garnett DJ. Caveolae as a target to quench autoinduction of the metastatic phenotype in lung cancer. J Cancer Res Clin Oncol. 2016 Mar;142(3):611-8.

[2]Jendželovský R, Jendželovská Z, Hiľovská L, Kovaľ J, Mikeš J, Fedoročko P. Proadifen sensitizes resistant ovarian adenocarcinoma cells to cisplatin. Toxicol Lett. 2016 Jan 22;243:56-66

[3]Grinchii D, Paliokha R, Tseilikman V, Dremencov E. Inhibition of cytochrome P450 by proadifen diminishes the excitability of brain serotonin neurons in rats. Gen Physiol Biophys. 2018 Sep;37(6):711-713

[4]Jendželovský R, Koval J, Mikeš J, Papčová Z, Plšíková J, Fedoročko P. Inhibition of GSK-3β reverses the pro-apoptotic effect of proadifen (SKF-525A) in HT-29 colon adenocarcinoma cells. Toxicol In Vitro. 2012 Sep;26(6):775-82

[5]Zygmunt PM, Edwards G, Weston AH, Davis SC, Högestätt ED. Effects of cytochrome P450 inhibitors on EDHF-mediated relaxation in the rat hepatic artery. Br J Pharmacol. 1996 Jul;118(5):1147-52

[6]Choo LK, Malta E, Mitchelson F. Investigation of the antimuscarinic and other actions of proadifen in-vitro. J Pharm Pharmacol. 1986 Dec;38(12):898-901

Proadifen HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.82mL

2.56mL

1.28mL

25.64mL

5.13mL

2.56mL

Proadifen HCl 技术信息

CAS号62-68-0
分子式C23H32ClNO2
分子量 389.959
别名 盐酸丙基解痉素 ;SKF-525A;U-5446;NSC 170997;SKF 525A (hydrochloride);RP-5171;Proadifen hydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解方案

DMSO: 50 mg/mL(128.22 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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