1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR Sigma Receptor
  3. NMDA receptor antagonist 9

NMDA receptor antagonist 9 是一种选择性靶向含 GluN2B 亚基的 NMDA 受体的拮抗剂,其 Ki 值为 5.2 nM。NMDA receptor antagonist 9 对 σ1 受体的选择性为 9 倍,但对 σ2 受体的选择性较差。NMDA receptor antagonist 9 可抑制含 GluN2B 亚基的 NMDA 受体的离子流。NMDA receptor antagonist 9 可用于神经系统疾病的研究,例如阿尔茨海默病和帕金森病。

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NMDA receptor antagonist 9

NMDA receptor antagonist 9 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NMDA receptor antagonist 9 is a selective GluN2B subunit-containing NMDA receptor antagonist with a Ki of 5.2 nM. NMDA receptor antagonist 9 exhibits 9-fold selectivity over σ1 receptors, shows poor selectivity towards σ2 receptors. NMDA receptor antagonist 9 inhibits ion flux through GluN2B subunit-containing NMDA receptors. NMDA receptor antagonist 9 can be used for the research of neurological disease, such as alzheimer’s disease and parkinson’s disease[1].

IC50 & Target[1]

GluN2B

5.2 nM (Ki)

σ2

4.2 nM (Ki)

σ1

49 nM (Ki)

体外研究
(In Vitro)

NMDA receptor antagonist 9 (Compound cis-15a) 在重组 L (tk-) 细胞中与含 GluN2B 亚基的 NMDA 受体结合,其 Ki 值为 5.2 ± 1.9 nM[1]
NMDA receptor antagonist 9 (1 μM) 可使非洲爪蟾 (Xenopus laevis) 卵母细胞中表达的含 GluN2B 亚基的 NMDA 受体的离子通量抑制 76±2%[1]
NMDA receptor antagonist 9 与豚鼠脑细胞膜中的 σ1 和 σ2 受体结合,其 Ki 值为 49 ± 7 和 4.2 ± 0.6 nM[1]
NMDA receptor antagonist 9 (90 min at 37 °C) 在小鼠肝微粒体中表现出较高的 I 相代谢稳定性,孵育后完整率为 89 ± 6%[1]
NMDA receptor antagonist 9 (90 min at 37 °C) 在含有 NADPH 和 UDP-GA 的小鼠肝微粒体中保留了较高的代谢稳定性,孵育后仍有 88% 保持完整[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

323.43

Formula

C21H25NO2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NMDA receptor antagonist 9
目录号:
HY-181007
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