Auglurant (C09-1102-723)

Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC 50 value of 11 nM (rat) and an IC 50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetrationIn VitroAuglurant (VU0424238) with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAuglurant (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:rat mGluR5 11 nM (IC 50 ) human mGluR5 14 nM (IC 50 ). Specifications and Purity: 99%. Molecular Formula: C16H12FN5O2. Molecular Weight: 325.30. PubChem CID: 60168069. Isomeric SMILES: CC1=CC(=CC(=N1)C(=O)NC2=NC=C(C=C2)F)OC3=CN=CN=C3.