VU6028418| ChemScene
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4.IC50 & Target:IC50: 4.1 nM (hM4 mAChR)In Vivo:VU6028418 is orally bioavailable.
In Vivo PK Parameters for VU6028418
| parameter | rat (SD)a |
mouse (CD-1)a |
dog (beagle)a |
| dose (mg/kg) iv/po | 1/10 | 1/3 | 1/3 |
| CLp (mL/min/kg) | 6.1 | 17 | 43 |
| Vss (L/kg) | 6.7 | 10.6 | 8.5 |
| elimination t1/2 (h) | 13 | NC | 15 |
| Cmax (ng/mL) po | 17 000 | 181 | 70 |
| Tmax (h) po | 1.5 | 6.67 | 17 |
| AUC0-inf (ng/mL?h) po | 30 000 | NC | 1100 |
| F (%) po | ≥100 | ≥100 | 86 |
| total brain/total plasma (Kp) | 6.4 | ND | ND |
| unbound brain/unbound plasma (Kp,uu) |
0.61 | ND | ND |
| CSF/plasma unbound (Kp,u) | 0.24 | ND | ND |
a Values represent means from two to three animals. ND = not determined. NC = not calculated; there was insufficient data to define the elimination phase (i.e., Cmax was one of the last three time points).
| Trivial name | VU6028418 |
| Catalog Number | CS-0201169 |
| Molecular Formula | 432.48 |
| CAS# | 2649803-05-2 |
| Purity | >98% |
| Condensed Formula | C23H27F3N4O |
| Size | 100mg |
| Supplier Page | www.chemscene.com/2649803-05-2.html |