For research use only. Not for therapeutic Use.
VU6001221 is a choline transporter (CHT) inhibitor (IC50 value of 270 nM) with comparable potency for choline uptake inhibition as ML352 (Axon 2587), yet improved PK and CNS penetration. For the first time, VU6001221 allowed evaluation of a CHT inhibitor in a standard preclinical rodent cognition model, namely novel object recognition (NOR).
KEYWORDS: VU6001221 | CHT inhibitor | VU 6001221 | VU-6001221 | CAS [2002495-17-0] | Choline | CHT | Inhibitor | Proteins
| Catalog Number | I047623 |
| CAS Number | 2002495-17-0 |
| Molecular Formula | C20H26ClN3O3 |
| Purity | ≥95% |
| IUPAC Name | 4-chloro-3-(1-methylpiperidin-4-yl)oxy-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]benzamide |
| InChI | InChI=1S/C20H26ClN3O3/c1-13(2)18-11-16(27-23-18)12-22-20(25)14-4-5-17(21)19(10-14)26-15-6-8-24(3)9-7-15/h4-5,10-11,13,15H,6-9,12H2,1-3H3,(H,22,25) |
| SMILES | CC(C)C1=NOC(=C1)CNC(=O)C2=CC(=C(C=C2)Cl)OC3CCN(CC3)C |
| Reference | JL Bertron et al. Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4637-40. |
