Auglurant,1396337-04-4

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Auglurant

CAS No. : 1396337-04-4

MCE 国际站：Auglurant

产品活性：Auglurant (VU0424238) 是一种新型的有选择性的 mGlu5 拮抗剂，抑制大鼠 mGlu5 的 IC₅₀ 值为 11 nM，人 mGlu5 的 IC₅₀ 值为 14 nM。Auglurant (VU0424238) 可渗透通过神经系统。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

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.

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