您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Radiprodil
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Radiprodil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Radiprodil图片
CAS NO:496054-87-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
RGH-896
产品介绍
Radiprodil 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。

产品描述

Radiprodil (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).

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].

Cas No.

496054-87-6

分子式

C21H20FN3O4

分子量

397.406

别名

RGH-896

储存和溶解度

DMSO:220 mg/mL (553.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years