| Identification | Back Directory | [Name]
VU 6008667 | [CAS]
2092923-21-0 | [Synonyms]
VU 6008667
5H-Imidazo[2,1-a]isoindol-5-one, 9b-(4-chloro-3-methylphenyl)-1-(3,4-difluorobenzoyl)-1,2,3,9b-tetrahydro-, (9bS)- | [Molecular Formula]
C24H17ClF2N2O2 | [MDL Number]
MFCD32174242 | [MOL File]
2092923-21-0.mol | [Molecular Weight]
438.85 |
| Chemical Properties | Back Directory | [Boiling point ]
616.1±55.0 °C(Predicted) | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mg/mL (227.87 mM) | [form ]
Solid | [pka]
-2.76±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration[1]. | [in vivo]
VU 6008667 (1 mg/kg)/PO (3 mg/kg, solution dose) displays a diminished elimination half-life (t1/2=2.3 hr) driven by a smaller volume (Vss=7.4 L/kg) and higher clearance (CLp=82 mL/min/kg), with moderate oral bioavailability (17% F)[1]. | Animal Model: | RAT (PK study)[1] | | Dosage: | 1 mg/kg; 3 mg/kg | | Administration: | oral adminstration | | Result: | Had a desired short half-life in rat (t1/2= 2.3 hr), with moderate oral bioavailability (17% F). |
| [IC 50]
mAChR5 | [References]
[1] McGowan KM et al, Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1356-1359. DOI:10.1016/j.bmcl.2017.02.020 |
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