货号:A900895
同义名:
FUT-187 free base
Sepimostat是通过拮抗 NR2B N-methyl-D-aspartate 受体而发挥神经保护作用,作用于 NR2B 亚基的 Ifenprodil 结合位点,抑制 Ifenprodil 结合的 Ki 值为 27.7 μM。


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| 产品名称 | AMPA receptor ↓ ↑ | GluR ↓ ↑ | mGluR5 ↓ ↑ | NMDA receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Evans Blue | ✔ | 85% (Dye content) | |||||||||||||||||
| IEM-1754 |
+
GluR3, IC50: 6 μM GluR1, IC50: 6 μM |
99% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | 99% | |||||||||||||||||
| (-)-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 | Sepimostat demonstrates neuroprotective effects through antagonism of the NR2B N-methyl-D-aspartate receptor at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits Ifenprodil binding with a Ki value of 27.7 µM [1]. |
| 体内研究 | Sepimostat (1 to 100 nmol/eye, intravitreal injection) demonstrates notable neuroprotective effects [1]. |
| Administration | Dosage | Frequency | Description | References | ||
| Rats | NMDA-induced retinal degeneration model | Intravitreal injection | 1 to 100 nmol/eye | Single injection | To evaluate the neuroprotective effect of Sepimostat against NMDA-induced retinal degeneration. Results showed that Sepimostat significantly inhibited NMDA-induced retinal degeneration at doses ranging from 1 to 100 nmol/eye. | Sci Rep. 2019 Dec 31;9(1):20409 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.68mL 0.54mL 0.27mL |
13.39mL 2.68mL 1.34mL |
26.78mL 5.36mL 2.68mL |
|
| CAS号 | 103926-64-3 |
| 分子式 | C21H19N5O2 |
| 分子量 | 373.41 |
| SMILES Code | O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC4=NCCN4)C=C3 |
| MDL No. | MFCD00868988 |
| 别名 | FUT-187 free base |
| 运输 | 蓝冰 |
| InChI Key | QMRJOIUGPCVZPH-UHFFFAOYSA-N |
| Pubchem ID | 108041 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 5 mg/mL(13.39 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 |
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