Proadifen HCl

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Chemical Structure| 62-68-0 同义名 : 盐酸丙基解痉素 ;SKF-525A;U-5446;NSC 170997;SKF 525A (hydrochloride);RP-5171;Proadifen hydrochloride
CAS号 : 62-68-0
货号 : A263311
分子式 : C23H32ClNO2
纯度 : 99%+
分子量 : 389.959
MDL号 : MFCD00055151
存储条件:

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

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
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].
实验方案
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

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