Auglurant

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^[1]. In Vitro: Auglurant (VU0424238) with an IC₅₀ value of 14 nM in HEK293A cells. It also binding a known allosteric site with K _i value of 4.4 nM in HEK293A cells. In Vivo: 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^[1].