Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Orphenadrine 是一种非竞争性的 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,以浓度依赖性方式抑制克隆的 HERG 通道,在 HEK 细胞中产生0.85μM 的 IC。Orphenadrine 是中枢和外周毒蕈碱受体的拮抗剂,通过孔残基 Y652或 F656突变阻断衰减。 Orphenadrine 具有抗痉挛、镇痛和抗胆碱能活性,对在体外和体内对谷氨酸神经毒性具有保护作用。Orphenadrine 对钠离子通道具有抑制作用,可用来治疗帕金森。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 315 | 现货 | ||
10 mg | ¥ 438 | 现货 | ||
25 mg | ¥ 697 | 现货 | ||
50 mg | ¥ 976 | 现货 | ||
100 mg | ¥ 1,580 | 现货 |
产品描述 | Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease. |
体外活性 | Orphenadrine decreased CYP2B6 marker activity up to 45-57% in human liver microsomes and up to 80-97% in cell microsomes containing cDNA-expressed CYP2B6. Orphenadrine strongly decreased CYP2D6 marker activity by 80-90%. Orphenadrine also partially decreased the CYP1A2, CYP2A6, CYP3A4, and CYP2C19 marker activities.[4] |
体内活性 | Orphenadrine (75 mg/kg/day; i.p.; for 3 days) was associated with a 2-fold induction of total hepatic P-450, a 5- and 2.4-fold induction of androstenedione 16 beta- and 6 beta-hydroxylase activity, respectively, and formation of an orphenadrine-P-450 MI complex. Western blots of orphenadrine-induced microsomes revealed a 20-fold increase in P-450 PB-B/D-immunoreactive protein.[2] |
别名 | Orphenadrine (free base) |
分子量 | 269.38 |
分子式 | C18H23NO |
CAS No. | 83-98-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (185.61 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.7122 mL | 18.5611 mL | 37.1223 mL | 92.8057 mL |
5 mM | 0.7424 mL | 3.7122 mL | 7.4245 mL | 18.5611 mL | |
10 mM | 0.3712 mL | 1.8561 mL | 3.7122 mL | 9.2806 mL | |
20 mM | 0.1856 mL | 0.9281 mL | 1.8561 mL | 4.6403 mL | |
50 mM | 0.0742 mL | 0.3712 mL | 0.7424 mL | 1.8561 mL | |
100 mM | 0.0371 mL | 0.1856 mL | 0.3712 mL | 0.9281 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。
Orphenadrine 83-98-7 Membrane transporter/Ion channel Neuroscience NMDAR AChR Sodium Channel Orphenadrine (free base) Inhibitor inhibitor inhibit