VU 6008667 (C09-1184-688)

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC 50 s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetrationIn VivoVU 6008667 (1 mg/kg)/PO (3 mg/kg, solution dose) displays a diminished elimination half-life (t 1/2 =2.3 hr) driven by a smaller volume (V ss =7.4 L/kg) and higher clearance (CL p =82 mL/min/kg), with moderate oral bioavailability (17% F) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: RAT (PK study) Dosage: 1 mg/kg; 3 mg/kg Administration: oral adminstration Result: Had a desired short half-life in rat (t 1/2 = 2.3 hr), with moderate oral bioavailability (17% F).Form:SolidIC50& Target:IC50: 1.2 μM (Human M5),1.6 μM (Rat M5). Specification: 0.98 Molecular Formula: C24H17ClF2N2O2 Molecular Weight: 438.85 PubChem CID: 134824563 Isomeric SMILES: CC1=C(C=CC(=C1)[C@@]23C4=CC=CC=C4C(=O)N2CCN3C(=O)C5=CC(=C(C=C5)F)F)Cl