产品
编 号:F745152
分子式:C21H22F3N5O2
分子量:433.43
产品类型
结构图
CAS No: 1432729-22-0
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产品详情
生物活性:
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
体内研究:
MK-8768 优先采用肌肉注射。MK-8768 (3 mg/kg, i.m, 2 times weekly) 在恒河猴ORD模型中明显改善东莨菪碱损伤后的影响,维持良好的执行功能和注意力。Animal Model:Rhesus monkey ORD model
Dosage: 3 mg/kg
Administration: Intramuscular (i.m.), 2 times weekly
Result:Improved object retrieval following scopolamine impairment obviously at the concentration of 0.3 mg/ml.
体外研究:
MK-8768 (40 n M, 5 min) 在过表达 mGluR2 的 CHOdhfr 细胞系中抑制 mGluR2 酶活,IC50值为0.9 nM。