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ML352
- VU0476201
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C21H29N3O4
- MW: 387.47
Description
ML352 (VU0476201) is a potent and selective inhibitor of the presynaptic choline transporter (CHT) with a Ki value 92 nM. ML352 exhibited no inhibition of acetylcholinesterase (AChE) or cholineacetyltransferase (ChAT) and also lacked activity at dopamine, serotonin, and norepinephrine transporters, as well as many receptors and ion channels. Because CHT is the rate-limiting factor in the recycling of choline, ML352 is a valuable tool for regulating acetylcholine (ACh) synthesis and studying cholinergic neurotransmission.
CHT pharmacology is relevant to addiction, schizophrenia, dystonia; ML352 supports mechanistic studies of CHT in biochemical, cellular and disease-model assays.
Key Features
- Highly potent and selective CHT inhibitor
- Ki: 92 nM
- Modulates CHT-dependent biological activity
- Blood-brain barrier penetrant for in vivo neuropharmacology studies
Applications
- CHT pharmacology and target-validation studies
- Disease-model research related to addiction, schizophrenia
- Transporter or ion-channel functional assays
More Information
| Parent CAS No. | 1649450-12-3 |
|---|---|
| Chemical Name | N-((3-isopropylisoxazol-5-yl)methyl)-4-methoxy-3-(1-methylpiperidin-4-yloxy)benzamide |
| SMILES | C(NCC1ON=C(C(C)C)C=1)(=O)C1=CC=C(OC)C(OC2CCN(C)CC2)=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H29N3O4/c1-14(2)18-12-17(28-23-18)13-22-21(25)15-5-6-19(26-4)20(11-15)27-16-7-9-24(3)10-8-16/h5-6,11-12,14,16H,7-10,13H2,1-4H3,(H,22,25) |
| InChiKey | WBLVOWHFRUAMCP-UHFFFAOYSA-N |
| CID | 70679283 |
| Short Description | CHT inhibitor |
References
- SR Bollinger et al. Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1757-60.
- EA Ennis et al. Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem Neurosci. 2015 Mar 18;6(3):417-27.
- 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.
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