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Radiprodil {[allProObj[0].p_purity_real_show]}

货号:A1142878 同义名: RGH-896

Radiprodil是一种选择性的 NMDA NR2B 拮抗剂,用于治疗神经病理性疼痛。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Radiprodil 化学结构 CAS号:496054-87-6
Radiprodil 化学结构
CAS号:496054-87-6
Radiprodil 3D分子结构
CAS号:496054-87-6
Radiprodil 化学结构 CAS号:496054-87-6
Radiprodil 3D分子结构 CAS号:496054-87-6
规格 价格 会员价 库存 数量
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Radiprodil 纯度/质量文件 产品仅供科研

货号:A1142878 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 NMDA receptor 其他靶点 纯度
Empirical Formula 97%
Dizocilpine maleate +++

NMDA receptor, Kd: 37.2 nM

99%+
Felbamate +

NMDAR, IC50: 1.8 mM

98%
(-)-Dizocilpine maleate ++++

NMDA receptor, Ki: 30.5 nM

98%
Ifenprodil tartrate +++

NMDA Receptor, IC50: 0.3 μM

98%
Spermidine Autophagy 98% GC
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Radiprodil 生物活性

描述 Radiprodil (RGH-896) is an orally active, selective NMDA NR2B antagonist, identified as a potential treatment for neuropathic pain and possibly other chronic pain conditions[1].
体内研究

Radiprodil blocks NMDA currents in Mg2+ insensitive variants with similar potencies to those without Mg2+[3].

Radiprodil demonstrates greater efficacy at pH 7.0 compared to pH 7.6, indicating its potential to sustain blockade of glutamate-induced NMDA currents amidst acidic conditions associated with prolonged seizures [3].

体外研究

Pre-treatment with Radiprodil (10 nM) restores long-term potentiation (LTP) affected by Aβ1-42, 3NTyr10-Aβ, and Aβ1-40, although not by AβpE3[2].

Regarding LTP, Radiprodil (10 nM) counteracts the synaptic toxicity caused by 3NTyr-Aβ, Aβ1-40, and Aβ1-42, but it does not affect the toxicity induced by AβpE3-42[2].

Radiprodil 参考文献

[1]Mony L, et al. Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential. Br J Pharmacol. 2009 Aug;157(8):1301-17.

[2]Rammes G, et al. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (Aβ) species on long-term potentiation (LTP). Neuropharmacology. 2018 Sep 15;140:184-192.

[3]Mullier B, et al. GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors. Neuropharmacology. 2017 Sep 1;123:322-331.

Radiprodil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

Radiprodil 技术信息

CAS号496054-87-6
分子式C21H20FN3O4
分子量 397.4
别名 RGH-896
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

溶解方案

DMSO: 250 mg/mL(629.09 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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