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533917 Choline Transporter Inhibitor II, ML352 - CAS 1649450-12-3 - Calbiochem

A moderately brain permeant, non-choline based highly selective and potent inhibitor of high-affinity choline transporter (CHT; Ki = 92 nM in hCHT-LV-AA transfected HEK293 cells).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-((3-Isopropylisoxazol-5-yl)methyl)-4-methoxy-3-((1-methylpiperidin-4-yl)oxy)benzamide, 4-Methoxy-3-(1-methylpiperidin-4-yl)oxy-N-((3-propan-2-yl-1,2-oxazol-5-yl)methyl)benzamide, CHT Inhibitor II, VU0476328

Primary Target: CHT
533917
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Overview

Key Spec Table

CAS #Empirical Formula
1649450-12-3C₂₁H₂₉N₃O₄

Products

Catalogue NumberPackaging Qty/Pack
5.33917.0001 Glass bottle 10 mg
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Description
OverviewA moderately brain permeant, non-choline based isoxazolylbenzamide compound that acts as a highly selective and potent inhibitor of high-affinity choline transporter (CHT; Ki = 92 nM in hCHT-LV-AA transfected HEK293 cells and 166 nM in mouse brain synaptosomes). The inhibition appears to be allosteric and noncompetitive. Does not affect the activity of acetylcholinesterase or cholineacetyltransferase and has no activity against dopamine, serotonin, and norepinephrine transporters. Also does not affect CHT protein expression. Exhibits high selectivity when tested against 68 GPCRs, ion channels, and transporters (IC50 > 10 µM). Displays moderate pharmacokinetic properties (t1/2= 33 min, AUC = 77.5 ng/h/ml; Cmax = 32.6 ng/ml, at 2.3 mg/kg, p.o. in Sprague-Dawley rats) and attractive solubility (98.2 µM in PBS). Does not affect the activity of cytochrome P450 and hERG (IC50 > 30 µM).
Catalogue Number533917
Brand Family Calbiochem®
SynonymsN-((3-Isopropylisoxazol-5-yl)methyl)-4-methoxy-3-((1-methylpiperidin-4-yl)oxy)benzamide, 4-Methoxy-3-(1-methylpiperidin-4-yl)oxy-N-((3-propan-2-yl-1,2-oxazol-5-yl)methyl)benzamide, CHT Inhibitor II, VU0476328
DescriptionCholine Transporter Inhibitor II, ML352
References
ReferencesEnnis, E.A., et al. ACS Chem. Neurosci. 6, In press.
Product Information
CAS number1649450-12-3
FormBrown solid
Hill FormulaC₂₁H₂₉N₃O₄
Chemical formulaC₂₁H₂₉N₃O₄
ReversibleY
Quality LevelMQ100
Biological Information
Primary TargetCHT
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
5.33917.0001 04055977281576