| Bioactivity | 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[1]. |
| Invitro | NP10679 (1-1000 nM) pH 依赖性地抑制 GluN2B，在 pH 6.9 和 7.6 时，IC50 分别为 23 和 142 nM[2]。NP10679 对 5-HT2A，α 肾上腺素受体-1A (α1A)，H1-组胺受体 (H1) 和 hERG 通道具有抑制作用，IC50 分别为 1.71，0.154，0.073 和 0.617 μM [2]。NP10679 对 5-HT1D，5-HT2A，5-HT2B，α1A，α1B，α1D，αa2C，H1-组胺受体 (H1) 和血清素转运蛋白 SERT 的 Ki 值分别为 2.29，0.638，1.92，0.603，1.92，0.495，3.09，0.040 和 0.135。 |
| In Vivo | NP10679 (2，5 和 10 mg/kg；腹腔注射，在短暂性缺血之前) 减少短暂性缺血小鼠的梗死体积[2]。 Animal Model: |
| Name | NP10679 |
| Formula | C23H26F3N3O3 |
| Molar Mass | 449.47 |
| 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]. Zaczek R, et al. Phase 1 Clinical Results for NP10679, a pH-sensitive GluN2B-selective N-methyl-d-aspartate Receptor Inhibitor. Clin Pharmacol Drug Dev. 2023 Jan 15. [2]. Myers SJ, et al. A Glutamate N-Methyl-d-Aspartate (NMDA) Receptor Subunit 2B-Selective Inhibitor of NMDA Receptor Function with Enhanced Potency at Acidic pH and Oral Bioavailability for Clinical Use. J Pharmacol Exp Ther. 2021 Oct;379(1):41-52. |