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Rislenemdaz {[allProObj[0].p_purity_real_show]}

货号:A709210 同义名: MK-0657;CERC-301

Rislenemdaz, also known as MK-0657, is a NR2B-selective NMDA antagonist potentially for the treatment of Parkinson's disease.

Rislenemdaz 化学结构 CAS号:808732-98-1
Rislenemdaz 化学结构
CAS号:808732-98-1
Rislenemdaz 3D分子结构
CAS号:808732-98-1
Rislenemdaz 化学结构 CAS号:808732-98-1
Rislenemdaz 3D分子结构 CAS号:808732-98-1
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Rislenemdaz 纯度/质量文件 产品仅供科研

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NMDAR, IC50: 1.8 mM

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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。
产品名称 AMPA receptor GluR mGluR5 NMDA receptor 其他靶点 纯度
Evans Blue 85% (Dye content)
IEM-1754 +

GluR1, IC50: 6 μM

GluR3, IC50: 6 μM

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AChE (G4 form), Ki: 7 nM

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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。

Rislenemdaz 生物活性

描述 Rislenemdaz, also known as CERC-301, inhibits calcium influx agonist-stimulated NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz is at least 1000-fold more selective for the GluN2B receptor compared to all targets tested, including hERG potassium channels. At 10 uM, Rislenemdaz is also minimally active against sigma-type receptors[1].

Rislenemdaz 动物研究

Animal study At doses of 1, 3, 10 and 30 mg/kg, Rislenemdaz significantly reduced immobility frequency and significantly increased swimming behaviour. At the time of sampling, plasma levels of Rislenemdaz were approximately 15, 120, 390, 1,420, 4,700, and 14,110 nM, which corresponded to approximately 5, 29, 56, 83, 94, and 98% of the RO in rats, respectively. The LD50s for the increase in swimming frequency and the decrease in immobility were approximately 0.3 and 0.7 mg/kg, which corresponded to approximately 30% and 50% of the RO. Rislenemdaz (1, 3, 10 and 30 mg/kg) significantly increased the total swimming distance compared to the control group in a 60-min test[1].

Rislenemdaz 参考文献

[1]Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198.

Rislenemdaz 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.40mL

27.90mL

5.58mL

2.79mL

Rislenemdaz 技术信息

CAS号808732-98-1
分子式C19H23FN4O2
分子量 358.41
别名 MK-0657;CERC-301
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(292.96 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

动物实验配方
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