产品
编 号:F149982
分子式:C16H12FN5O2
分子量:325.3
产品类型
结构图
CAS No: 1396337-04-4
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产品详情
生物活性:
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
体内研究:
Auglurant (VU0424238) had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monkeys and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons.
体外研究:
Auglurant (VU0424238) with an IC50 value of 14 nM in HEK293A cells. It also binding a known allosteric site with K ivalue of 4.4 nM in HEK293A cells.