NP10679

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NP10679 是一种选择性、pH 依赖性的 GluN2B 亚基 特异的 N-methyl-D-aspartate (NMDA) 受体抑制剂，具有较高的口服生物利用度和良好的脑穿透性。NP10679 在 pH 6.9 和 7.6 下，抑制 GluN2B 的 IC50 分别为 23 和 142 nM。NP10679 是 histamine H1 的拮抗剂和 hERG 通道抑制剂，IC50 分别为 73 和 620 nM。NP10679 是一种可逆的人肝脏 CYP 酶抑制剂。

NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.

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Animal Model:Male C57BL/6 middle cerebral artery occlusion (MCAo) model of transient ischemia mice Dosage:2, 5 and 10 mg/kg Administration:Intraperitoneal injection; 2, 5 and 10 mg/kg, 15 minutes prior to transient ischemia Result:Dose-dependently reduced infarct volumes with an ED50 of 1 mg/kg.

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Angiogenesis

HER/HSP

HER | P450 | Histamine Receptor | NMDAR

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2914889-88-4

449.47

C23H26F3N3O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (222.48 mM; 超声助溶 )

O(C[C@@H](CN1CCN(CC1)C2=CC=C(C(F)(F)F)C=C2)O)C=3C=C4C(=CC3)NC(=O)CC4

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(-20℃)

With Ice Pack

≥ 2 years