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.
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- CAS No.: 2002495-17-0
- Formule: C20H26ClN3O3
- Masse moléculaire:391.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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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Masse moléculaire 391.89
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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)
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