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VU6001221
- Soluble in DMSO
- MF: C20H26ClN3O3
- MW: 391.89
Description
VU6001221 is a centrally penetrant, high-affinity choline transporter (CHT) inhibitor, with an IC50 of 270 nM for inhibition of choline uptake. It retains potency comparable to ML352 (Axon 2587) while providing improved pharmacokinetic properties and brain exposure. By limiting CHT-mediated choline recycling, VU6001221 enables pharmacological investigation of the rate-limiting step in acetylcholine synthesis.
VU6001221 is a refined in vivo chemical probe for cholinergic neuroscience, validated in the rodent novel object recognition paradigm. It is useful for studying presynaptic cholinergic tone, acetylcholine-dependent cognition, transporter pharmacology, and the relationship between CHT function and behavioral performance.
Key Features
- Potent and selective CHT inhibitor
- IC50: 270 nM for inhibition of choline uptake
- Improved pharmacokinetics and brain penetration
- Suitable for cellular and in vivo cholinergic studies
Applications
- Choline transporter pharmacology
- Acetylcholine synthesis and presynaptic cholinergic signaling
- Cognition and novel object recognition studies
- CNS pharmacokinetic and target-engagement research
More Information
| Parent CAS No. | 2002495-17-0 |
|---|---|
| Chemical Name | 4-Chloro-N-((3-isopropylisoxazol-5-yl)methyl)-3-(1-methylpiperidin-4-yloxy)benzamide |
| SMILES | C1(Cl)C(OC2CCN(C)CC2)=CC(C(=O)NCC2=CC(C(C)C)=NO2)=CC=1 |
| MFCD | N.A. |
| 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) |
| InChiKey | IMOCLELOJXGLLE-UHFFFAOYSA-N |
| CID | 129909861 |
| Short Description | CHT inhibitor |
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