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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 | The N-methyl-D-aspartate receptors (NMDARs) are ionotropic glutamate (iGlu) receptors essential for glutamate excitotoxicity. They play important roles in synaptic plasticity and cell survival. NMDAR antagonist 1 is a potent, orally bioavailable NMDAR antagonist. The viability of SH-SY5Y cells treated with 0.1, 1, 10, and 100 µM NMDAR antagonist 1 was 75.8%, 80.0%, 84.4%, and 78.6%, respectively. NMDAR antagonist 1 at a concentration of 10 μM inhibited NMDA (2 nM)-induced influx of Ca2+ in SH-SY5Y cells. It also suppressed the upregulation of NR2B and increased p-ERK1/2 expression. NMDAR antagonist 1 exhibited high metabolic stability with a clearance rate of 46.3 μL/min/mg in human liver microsomes[1]. |
作用机制 | NMDAR antagonist 1 is a NR2B-selective NMDAR antagonist. It docks at the NR1-NR2B subunit interface[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.07mL 2.41mL 1.21mL |
24.14mL 4.83mL 2.41mL |
CAS号 | 2220162-06-9 |
分子式 | C20H20BrN3O2 |
分子量 | 414.296 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 | |
动物实验配方 |