| Description | MK-8768 is a potent, selective, and orally bioavailable negative allosteric modulator of the mGluR2 class, exhibiting an IC50 of 9.6 nM and characterized by excellent brain permeability. |
| In vitro | MK-8768(40 nM, 5分钟)在高表达mGluR2的CHOdhfr细胞系中显著抑制mGluR2的酶活性,其IC50为0.9 nM [1]。 |
| In vivo | MK-8768优先通过肌肉注射途径给药[1]。在恒河猴ORD模型中,MK-8768(3 mg/kg,i.m,每周2次)明显缓解了东莨菪碱引起的损害,保持了较好的执行功能和注意力水平[1]。 |
| molecular weight | 433.43 |
| Molecular formula | C21H22F3N5O2 |
| CAS | 1432729-22-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |