533917 Choline Transporter Inhibitor II, ML352 - Calbiochem

533917
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₂₉N₃O₄

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      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
      FormBrown solid
      Hill FormulaC₂₁H₂₉N₃O₄
      Chemical formulaC₂₁H₂₉N₃O₄
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCHT
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Choline Transporter Inhibitor II, ML352 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Ennis, E.A., et al. ACS Chem. Neurosci. 6, In press.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-September-2016 JSW
      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
      DescriptionA cell-permeable pyridinylpropanylthiophene-carboxamide compound that exhibits selective affinity toward MT/microtubule-bound KIFC1 motor domain (Q305-K673; Kd = 690 nM), but not to uncomplexed KIFC1 or MT, and selectively inhibits MT-induced, but not basal, KIFC1 motor domain ATPase activity (IC50 = 300 nM; [KIFC1] = 30 nM, [MT] = 100 nM, [ATP] = 15 µM) in an ATP-competitive (Ki = 43 nM; [KIFC1] = 125 nM, [MT] = 1.5 µM) and MT-noncompetitive manner, effectively preventing ADP release, while displaying little potency against 9 other kinesin motor proteins (<15% or no inhibition at 5 µM against human CENP-E, Chromokinesin/KIF4A, Eg5, KIFC3, KIF3C, KInesin Heavy Chain/KIF5B, MCAK/KIF2C, MKLP1/KIF23, and A. nidulans BimC/KIF8). KIFC1 knockdown by siRNA or functional inhibition by AZ82 (0.4 to 1.2 µM) is shown to result in mitotic delay and multipolar spindle formation among BT549 population with extra centrosomes due to failure of chromosomes clustering. In cells with normal/two centrosomes, Eg5 inhibition causes monopolar spindles formation, while AZ82 co-treatment (400 nM) offsets the effect of Eg5 inhibition (5 nM AZD4877) and restores bipolar spindles phenotype in mitotic HeLa cells. Off-target cytotoxicity is reported when used at concentrations above 4 µM.
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₂₉N₃O₄
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesEnnis, E.A., et al. ACS Chem. Neurosci. 6, In press.