| Bioactivity | 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]. |
| Invitro | 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. 0 --> GluN2B-NMDAR antagonist-2 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| 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: |
| Formula | C24H25Cl2N3O3 |
| Molar Mass | 474.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lin G, et al. Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment. J Med Chem. 2024 Feb 27. |
GluN2B-NMDAR antagonist-2
CAS: F: C24H25Cl2N3O3 W: 474.38
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagoni
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