Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
500 mg | ¥ 249 | 待询 | ||
1 g | ¥ 418 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 148 | 现货 |
产品描述 | Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen. |
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]。 |
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. |
别名 | 苯氧苯札明, NCI-c01661, NSC 37448, 盐酸酚苄明, Phenoxybenzamine HCl |
分子量 | 340.3 |
分子式 | C18H23Cl2NO |
CAS No. | 63-92-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 63 mg/mL (185.1 mM)
H2O: 14 mg/mL (41.1 mM)
DMSO: 55 mg/mL (161.62 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / H2O / DMSO | 1 mM | 2.9386 mL | 14.6929 mL | 29.3858 mL | 73.4646 mL |
5 mM | 0.5877 mL | 2.9386 mL | 5.8772 mL | 14.6929 mL | |
10 mM | 0.2939 mL | 1.4693 mL | 2.9386 mL | 7.3465 mL | |
20 mM | 0.1469 mL | 0.7346 mL | 1.4693 mL | 3.6732 mL | |
Ethanol / DMSO | 50 mM | 0.0588 mL | 0.2939 mL | 0.5877 mL | 1.4693 mL |
100 mM | 0.0294 mL | 0.1469 mL | 0.2939 mL | 0.7346 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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