For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I018781 |
| CAS Number | 2092923-21-0 |
| Synonyms | (9bS)-9b-(4-chloro-3-methylphenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydroimidazo[2,1-a]isoindol-5-one |
| Molecular Formula | C24H17ClF2N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H17ClF2N2O2/c1-14-12-16(7-8-19(14)25)24-18-5-3-2-4-17(18)23(31)29(24)11-10-28(24)22(30)15-6-9-20(26)21(27)13-15/h2-9,12-13H,10-11H2,1H3/t24-/m0/s1 |
| InChIKey | XMSLRELXMCKGCB-DEOSSOPVSA-N |
| SMILES | CC1=C(C=CC(=C1)C23C4=CC=CC=C4C(=O)N2CCN3C(=O)C5=CC(=C(C=C5)F)F)Cl |
| Reference | [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. |
