Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Radiprodil (RGH-896) 是一种具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。它有用于神经性疼痛和其它慢性疼痛的相关研究潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 588 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 4,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 995 | 现货 |
产品描述 | Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP). |
靶点活性 | NR2B:69 nM |
体外活性 | The inhibition potency of ligands toward the NR2B NMDA receptors was evaluated by measuring the Ca2t influx evocated by NMDA application (at 100 mM for 30 s) in NR1a/NR2B subunit transfected HEK cells. Radiprodil had potent inhibitory effects (69 nM) towards Ca2+ influx [1]. A low concentration (10?nM) of the GLUN2B receptor antagonist Radiprodil restored LTP in the presence of Aβ1-42, 3NTyr10-Aβ, Aβ1-40, but not AβpE3. Radiprodil (10?nM) reversed the synaptic toxicity of Aβ species but not that of AβpE3 [2]. |
体内活性 | The in vivo analgesic efficiency for 1a in the mouse formalin test was 7.7 mg/kg p.o. (ED50) and a clinical trial is currently conducted with Radiprodil [1]. |
别名 | RGH-896 |
分子量 | 397.4 |
分子式 | C21H20FN3O4 |
CAS No. | 496054-87-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 220 mg/mL (553.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5164 mL | 12.5818 mL | 25.1636 mL | 62.9089 mL |
5 mM | 0.5033 mL | 2.5164 mL | 5.0327 mL | 12.5818 mL | |
10 mM | 0.2516 mL | 1.2582 mL | 2.5164 mL | 6.2909 mL | |
20 mM | 0.1258 mL | 0.6291 mL | 1.2582 mL | 3.1454 mL | |
50 mM | 0.0503 mL | 0.2516 mL | 0.5033 mL | 1.2582 mL | |
100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6291 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。
Radiprodil 496054-87-6 Membrane transporter/Ion channel Neuroscience NMDAR iGluR Ionotropic glutamate receptors RGH-896 RGH896 inhibit Inhibitor RGH 896 inhibitor