530351 Nrf2 Activator IV, VSC2 - Calbiochem

530351
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₃ClO₃S

      Pricing & Availability

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      5.30351.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable vinylsulfone that acts as a more potent Nrf-2 activator than the chalcones (e.g. Cat. No. 492040) in stimulating HO-1 expression in murine microglial BV-2 cultures (3.82-fold of control in 24 h; 20 µM). Shown to induce overall Nrf2 cellular accumulation & nuclear translocation (1 to10 µM) in murine dopaminergic CATH.a cultures, presumably by freeing Nrf2 from its negative regulator keap1, with concomitant upregulation of Nrf2-regulated antioxidant enzymes expression, effectively protecting CATH.a against BH4 toxicity (effective conc. 0.1 to 1.0 µM against 200 µM BH4; 24 h) in vitro and preventing MPTP- (Cat. No. 506382) induced motor dysfunctions and neurodegeneration in a murine PD model in vivo (3X 10 mg drug/kg/d p.o.; 4X 20 mg MPTP/kg/2 h i.p.).
          Catalogue Number530351
          Brand Family Calbiochem®
          Synonyms(E)-1-Chloro-2-(2-(2-methoxyphenylsulfonyl)vinyl)benzene, Nuclear Factor E2-related Factor 2 Activator IV, VSC2
          References
          ReferencesLee, J.A., et al. 2015. Br. J. Pharmacol. 172, 1087.
          Woo, S.Y., et al. 2014. J. Med. Chem. 57, 1473.
          Product Information
          FormOff-white solid
          Hill FormulaC₁₅H₁₃ClO₃S
          Chemical formulaC₁₅H₁₃ClO₃S
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% 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

          Nrf2 Activator IV, VSC2 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Lee, J.A., et al. 2015. Br. J. Pharmacol. 172, 1087.
          Woo, S.Y., et al. 2014. J. Med. Chem. 57, 1473.
          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.

          Revision27-March-2015 JSW
          Synonyms(E)-1-Chloro-2-(2-(2-methoxyphenylsulfonyl)vinyl)benzene, Nuclear Factor E2-related Factor 2 Activator IV, VSC2
          DescriptionA cell-permeable vinylsulfone compound that acts as a more potent Nrf-2 activator than the analogous α,β-unsaturated ketone-based chalcones (e.g. Cat. No. 492040) in stimulating HO-1 expression in murine microglial BV-2 cultures (382% of control protein level in 24 h; 20 µM). Drug treatment in murine dopaminergic (DAergic) CATH.a cultures likewise effectively induces Nrf2 nuclear translocation (Fold of control in 3 h/dose = 1.4/1 µM, 2.3/5 µM, 3.4/10 µM) and overall Nrf2 cellular accumulation (Fold of control in 24 h/dose = 1.5/0.5 µM, 2.0/1 µM, 2.8/2 µM, 4.3/5 µM), presumably by freeing Nrf2 from its negative regulator keap1, with concomitant upregulation of Nrf2-regulated antioxidant enzymes expression, including heme oxygenase-1/OH-1, NAD(P)H quinone oxidoreductase 1/NQO1, glutamate-cysteine ligase modifier & catalytic subunits, QCLM & GCLC. Shown to protect CATH.a against BH4 toxicity (effective conc. 0.1 to 1.0 µM against 200 µM BH4 for 24 h) in vitro and prevent MPTP- (Cat. No. 506382) induced motor deficits/dysfunctions (by vertical grid test 6 d post MPTP injection) and neurodegeneration (by TH staining 7 d post MPTP injection) in a murine PD model in vivo (3 X 10 mg drug/kg/d oral dosages; 4X 20 mg MPTP/kg/2 h i.p. dosages starting 24 h post the 1st drug dosage).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₅H₁₃ClO₃S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          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
          ReferencesLee, J.A., et al. 2015. Br. J. Pharmacol. 172, 1087.
          Woo, S.Y., et al. 2014. J. Med. Chem. 57, 1473.