Bioactivity | 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]. |
Target | IC50: 1.2 μM (Human M5); 1.6 μM (Rat M5) |
In Vivo | VU 6008667(1 mg/kg或者3mg/kg,口服作用于大鼠)较小的体积(Vss = 7.4 L/kg)和较高的清除率,显示半衰期为2.3小时(t1/2 = 2.3 hr),CLp = 82 mL/min/kg,显示口服生物利用度为17%(17%F)[1]。 Animal Model: |
Name | VU 6008667 |
CAS | 2092923-21-0 |
Formula | C24H17ClF2N2O2 |
Molar Mass | 438.85 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
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. |