盐酸酚苄明 T1158

Product Introduction
Bioactivity


英文名: Phenoxybenzamine hydrochloride

描述: Phenoxybenzamine hydrochloride (NCI-c01661) 是一种选择性的 α-adrenoceptor 和 calmodulin 的抑制剂，是常用的抗高血压药。

细胞实验: Phenoxybenzamine hydrochloride is dissolved in DMSO. After cytometry, 1×3 cells are implanted in a 96-well plate in 100 μL DMEM supplemented with 10 % FBS. Ten microliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37°C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The mean fluorescence value is counted, and the cell number is determined using the standard curve.

体外活性: Phenoxybenzamine hydrochloride对[3H]yohimbine结合的阻断所导出的IC50（100 nM）明显低于其对Noradrenaline 引起的环磷酸腺苷（cyclic AMP）积累效应的逆转IC50（550 nM）[1]。Phenoxybenzamine hydrochloride（50 nM）与Phenoxybenzamine hydrochloridetolamine（1000 nM）联合使用比单独使用Phenoxybenzamine hydrochloride（50 nM）时更能增强Phenoxybenzamine hydrochlorideylephrine诱导的血管收缩，这一效果在完整内皮的主动脉中同样观察到。无论是dexmedetomidine（300或1000 nM）与Phenoxybenzamine hydrochloride（50 nM）的联合使用，还是Phenoxybenzamine hydrochloridetolamine（1000 nM）与Phenoxybenzamine hydrochloride（50 nM）的联合处理，相比单独使用Phenoxybenzamine hydrochloride（50 nM），都能增强Phenoxybenzamine hydrochlorideylephrine引发的收缩反应。此外，与dexmedetomidine（1000 nM）和Phenoxybenzamine hydrochloride的联合使用相比，Phenoxybenzamine hydrochloridetolamine与Phenoxybenzamine hydrochloride的联合使用在增强Phenoxybenzamine hydrochlorideylephrine引起的收缩方面更为显著。高浓度dexmedetomidine（1000 nM）与Phenoxybenzamine hydrochloride的联合使用，比低浓度dexmedetomidine（300 nM）与Phenoxybenzamine hydrochloride的联合使用，更能增强Phenoxybenzamine hydrochlorideylephrine诱发的收缩作用[2]。

体内活性: Phenoxybenzamine hydrochloride（20 nM，皮下注射）有效抑制了小鼠中胶质瘤细胞的肿瘤生成，且Phenoxybenzamine hydrochloride-U87 mg移植瘤的细胞密度显著下降[3]。以Phenoxybenzamine hydrochloride（1 mg/kg，静脉注射）处理的大鼠在神经症状打分（NSS）和足失误评分方面显示出显著改善[4]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 63 mg/mL (185.1 mM)
H2O : 14 mg/mL (41.1 mM)
DMSO : 63 mg/mL (185.1 mM)


关键字: Phenoxybenzamine hydrochloride | pheochromocytoma | Beta Receptor | neuroprotective | Phenoxybenzamine Hydrochloride | Inhibitor | Phenoxybenzamine | antitumor | NSC37448 | Adrenergic Receptor | hypertension | NSC-37448 | inhibit | glioma

相关产品: KN-93 Phosphate | STO-609 acetate | Calmidazolium chloride | Syntide 2 acetate(108334-68-5 free base) | KN-92 phosphate | Y-33075 dihydrochloride | W-5 hydrochloride | Trifluoperazine dihydrochloride | Calmodulin-Dependent Protein Kinase II 290-309 acetate | NH125

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | GPCR Compound Library | Highly Selective Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途