VU6001221
VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex.
For research use only. We do not sell to patients.
- CAS No.: 2002495-17-0
- Formula: C20H26ClN3O3
- Molecular Weight:391.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
270 nM
Compound: 4c; VU6001221
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Inhibition of [3H]choline uptake at human choline transporter expressed in HEK293 cells preincubated for 15 mins followed by [3H]choline addition measured after 10 to 15 mins by scintillation proximity assay
Inhibition of [3H]choline uptake at human choline transporter expressed in HEK293 cells preincubated for 15 mins followed by [3H]choline addition measured after 10 to 15 mins by scintillation proximity assay
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[PMID: 27575469] |
Chemical Information
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CAS No. 2002495-17-0
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Molecular Weight 391.89
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Formula C20H26ClN3O3
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SMILES
O=C(NCC1=CC(C(C)C)=NO1)C2=CC=C(Cl)C(OC3CCN(C)CC3)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Bertron JL, 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):4637-4640. [Content Brief]
[2]. Koshy Cherian A, et al. Unresponsive Choline Transporter as a Trait Neuromarker and a Causal Mediator of Bottom-Up Attentional Biases. J Neurosci. 2017 Mar 15;37(11):2947-2959. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU6001221 Related Classifications
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