2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. GluN2B-NMDAR antagonist-2

GluN2B-NMDAR antagonist-2 (compound S-58) 是一种有效的、选择性的、可穿过血脑屏障的 NMDAR-GluN2B 拮抗剂，IC50 值为74.01 nM。GluN2B-NMDAR antagonist-2 显示出轻微的细胞毒性。GluN2B-NMDAR antagonist-2 降低脑梗死率和神经功能缺损评分。GluN2B-NMDAR antagonist-2 具有研究中风的潜力。

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GluN2B-NMDAR antagonist-2 Chemical Structure

GluN2B-NMDAR antagonist-2 Chemical Structure

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GluN2B-NMDAR antagonist-2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke[1].

IC50 & Target

GluN2B

74.01 nM (IC50)

体外研究
(In Vitro)

GluN2B-NMDAR antagonist-2 (compound S-58) (1, 3, 10 µM) 对 hiPSC-CM 的动作电位持续时间 (APD90) 无显着延长作用[1]。
GluN2B-NMDAR antagonist-2 (0-300 µM; 48 h) 对原代小鼠神经元、VERO、L929、HEK293 细胞显示出轻微的细胞毒性[1]。

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

GluN2B-NMDAR antagonist-2 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: primary mouse neuron, VERO, L929, HEK293 cells
Concentration: 0, 0.3, 1, 3, 10, 100, 300 µM
Incubation Time: 48 h
Result: Showed mild cytotoxicity for primary mouse neuron, VERO, L929, HEK293 cells with IC50s of >300, 109.66, 56.34, 22.01 µM, respectively.
体内研究
(In Vivo)

GluN2B-NMDAR antagonist-2 (5, 10, 20 mg/kg; i.v.) 可在 MCAO 大鼠模型中以剂量依赖性方式降低脑梗死率和神经功能缺损评分[1]。
GluN2B-NMDAR antagonist-2 (450, 900 mg/kg; i.v.) 在 ICR 小鼠中表现出良好的安全性，最大耐受剂量 (MTD) 为 450 mg/kg[1]。

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

Animal Model: Fifty-six Sprague-Dawley rats (MCAO rat model)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.v.
Result: Significantly decreased the cerebral infarction rates and neurologic deficit scores in a dose dependent manner, dramatically improved motor function, decreased cerebral infarct volume, and reduced neurologic scores, significantly reduced the Ca2+ concentration in brain tissue.
分子量

474.38

Formula

C24H25Cl2N3O3
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

GluN2B-NMDAR antagonist-2 相关分类

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  • 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.

Keywords:

GluN2B-NMDAR antagonist-2iGluRIonotropic glutamate receptorsVEROL929HEK293 cellanti-strokeMCAO rat modelblood-brain barrierInhibitorinhibitorinhibit

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