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My CartCAS：63-92-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 63-92-3 |
| Name | Phenoxybenzamine Hydrochloride |
| Molecular Formula | C18H22ClNO·HCl |
| Molecular Weight | 340.3 |
| Solubility | Soluble in DMSO ≥5mg/mL;Soluble in Water ＜ 1mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-569-7 |
| MDL | MFCD00599580 |
| SMILES | CC(COC1=CC=CC=C1)N(CCCl)CC2=CC=CC=C2.Cl |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling |
| Background | Phenoxybenzamine Hydrochloride is a selective inhibitor of alpha-adrenoceptor and calmodulin. |
| Biological Activity | Phenoxybenzamine hydrochloride 是具有选择行的 α-adrenoceptor 和 calmodulin 的抑制剂，是一种常用的抗高血压药。[1-4] |
| In Vitro | 由苯氧基苯甲胺盐酸盐阻断[3H]育亨宾的IC50(100 nM)明显低于盐酸苯氧苄胺对环磷酸腺苷累积影响的相应逆转IC50(550 nM)[1]。苯氧苄胺盐酸盐(50 nM)与苯氧基苯甲胺盐酸胺(1000 nM)相结合，与在内皮完整主动脉中单独使用苯氧基苯甲胺盐酸盐(50 nM)预处理相比，增强了苯氧苄胺盐酸盐去氧肾上腺素诱导的收缩。与单独的苯氧基苯甲胺盐酸盐(50nM)相比，用右美托咪定(300或1000nM)和苯氧基苯甲胺盐酸盐(50nM)或苯氧基苯甲胺盐酸盐(1000nM)和苯氧基苯甲胺盐酸盐(50nM)的联合处理增强了苯氧基苯甲胺盐酸盐酰胺诱导的收缩。此外，与右美托咪定(1000 nM)和盐酸苯氧苄胺联合处理相比，与苯氧基苯甲胺盐酸胺和盐酸苯氧基苯甲胺的联合处理增强了苯氧基苯甲胺盐酸去氧肾上腺素诱导的收缩。与低浓度右美托咪定(300 nM)和盐酸苯氧苄胺联合治疗相比，高浓度右美托咪定(1000 nM)和盐酸苯氧苄胺联合治疗可增强苯氧苄胺盐酸盐去氧肾上腺素诱导的收缩[2]。苯氧苄胺盐酸盐(0.1-100μM)抑制胶质瘤增殖，迁移和侵袭，并抑制肿瘤发生能力。苯氧基苯甲胺盐酸盐也抑制胶质瘤干细胞样细胞的自我更新。 Phenoxybenzamine hydrochloride激活LINGO-1并抑制TrkB-Akt通路[3]。苯氧苄胺盐酸盐(0.1μM-1 mM)可保留CA1，CA3和齿状回内的原代神经元，并产生强大的神经保护作用，并在分娩后2，4和8小时分娩时防止海马区域内OGD神经元死亡-OGD为100μM[4]。 |
| In Vivo | 苯氧苄胺盐酸盐(20 nM，sc)有效抑制小鼠胶质瘤细胞的肿瘤发生，苯氧苄胺盐酸盐-U87MG异种移植物的细胞密度显著降低[3]。苯氧苄胺盐酸盐(1 mg / kg，iv)处理的大鼠在NSS和足部缺陷评分方面显示出显著改善[4]。 |
| Cell Experiment | 细胞计数后，将1×3细胞植入96孔板中的100μL补充有10％FBS的DMEM中。将10微升(总体积的10％)WST-1(水溶性四唑鎓)加入细胞中并在37℃下孵育30分钟，然后进行比色测定，以450nm激发和630nm发射，间隔24小时，直至96小时。 。计算平均荧光值，并使用标准曲线确定细胞数。 |
| Animal Experiment | 将U87MG细胞以每侧2.0×3 /200μL的剂量皮下注射到裸鼠的两侧。注射后8天，在小鼠的两侧肉眼观察到肿瘤生长。然后，以2天的间隔将20nM苯氧基苯甲胺盐酸盐皮下注射到右侧，并将溶剂DMSO用作对照。通过测量长度(a)和宽度(b)确定肿瘤体积(V)并使用以下等式计算：V =(ab)2/2。 |
| Data Literature Source | [1]. Lenox，R.H.，et al，Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve. Mol Pharmacol，1985. 27(1): p. 1-9. [2]. Byon HJ，et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017 Feb 7;14(2):143-149. [3]. Lin XB，et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8. [4]. Rau TF，et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int J Mol Sci. 2014 Jan 20;15(1):1402-17. |
| Unit | Bottle |
| Specification | 250mg 500mg |
是具有选择性的 α-adrenoceptor 和 calmodulin 的抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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