GluN2B-NMDAR antagonist-1_product_DataBase

Bioactivity	GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury[1].
Invitro	GluN2B-NMDAR antagonist-1 (Compound Z25) (0.05 μM, 0.5 μM, 5 μM) 在 SH-SY5Y 细胞中对 NMDA 诱导的细胞损伤显示出 35.7%、48.8%、55.8% 的神经保护百分比[1].GluN2B-NMDAR antagonist-1 (5 μM) 减少 NMDA (500 μM) 诱导的 SH-SY5Y 细胞中的 Ca2+ 内流[1]。GluN2B-NMDAR antagonist-1 (0.05-5 μM, 6 h) 增加 NMDA 诱导的 SH-SY5Y 细胞中 p-ERK1/2 表达的下调[1]。GluN2B-NMDAR antagonist-1 具有良好的血浆稳定性，半衰期值大于 289.1 分钟[1]。 Western Blot Analysis[1] Cell Line:
In Vivo	GluN2B-NMDAR antagonist-1 (Compound Z25) (20-80 mg/kg，灌胃) 改善 ICV-ET1 诱导的血管性痴呆小鼠模型中小鼠的认知能力[1]。 Animal Model:
Name	GluN2B-NMDAR antagonist-1
Formula	C26H23BrN2O2
Molar Mass	475.38
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]. Quan J,et al. Discovery of novel tryptamine derivatives as GluN2B subunit-containing NMDA receptor antagonists via pharmacophore-merging strategy with orally available therapeutic effect of cerebral ischemia. Eur J Med Chem. 2023 May 5;253:115318.

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