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.
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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。 |
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 |
99% | |||||||||||||||||
Latrepirdine 2HCl | ✔ | 98% | |||||||||||||||||
(-)-Huperzine A |
+++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
CTEP |
++++
mGlu5, IC50: 2.2 nM |
98%+ | |||||||||||||||||
MPEP |
++
mGluR5, IC50: 36 nM |
99%+ | |||||||||||||||||
Riluzole | ✔ | 97% | |||||||||||||||||
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。 |
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]. |
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]. |
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 |
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 |