533917 Choline Transporter Inhibitor II, ML352 - Calbiochem

533917
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₁H₂₉N₃O₄

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33917.0001
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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
          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.