Radiprodil|496054-87-6|(RGH-896)-陌孚医药/Medlife

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Radiprodil (Synonyms: RGH-896)

目录号: PL04227 纯度: ≥99%

CAS No. :496054-87-6

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中文名称	Radiprodil
英文名称	Radiprodil
英文别名	1-Piperidineacetamide, N-(2,3-dihydro-2-oxo-6-benzoxazolyl)-4-[(4-fluorophenyl)methyl]-α-oxo-;2-[4-(4-Fluorobenzyl)piperidin-1-yl]-2-oxo-N-(2-oxo-2,3-dihydrobenzoxazol-6-yl)acetamide;Radiprodil;2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]-2-oxo-N-(2-oxo-3H-1,3-benzoxazol-6-yl)acetamide;RGH 896 - RADIPRODIL
Cas No.	496054-87-6
分子式	C₂₁H₂₀N₃O₄F
分子量	397.40
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Radiprodil (RGH-896) 是具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。Radiprodil 有潜力用于神经性疼痛和其它慢性疼痛的相关研究。

生物活性

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.

性状

Solid

IC50 & Target[1][2]

NMDA NR2B.

体外研究(In Vitro)

Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ1-42, 3NTyr10-Aβ and Aβ1-40, but not AβpE3.
As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Radiprodil could block NMDA currents in Mg insensitive variants, with potencies similar to those obtained without Mg.
Radiprodils potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability to block glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 250 mg/mL (629.09 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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