532336 NOX Inhibitor VIII, VAS3947 - Calbiochem

532336
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₄H₁₀N₆OS

      Pricing & Availability

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      5.32336.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable triazolo-pyrimidine derivative of VAS2870 (Cat. No. 492000) that displays enhanced solubility and acts as a selective inhibitor NOX family of NADPH oxidase. Shown to inhibit NOX activity in CaCo-2 cells (expressing NOX 1, 2, 4, and 5; IC50 = 12 µM), HL-60 cells (mainly expressing NOX2; IC50 = 2 µM), and A7r5 cells (mainly expressing NOX3 and 4; IC50 = 13 µM). Does not affect the activities of xanthine oxidase and endothelial nitric oxide synthase (eNOS) even at higher concentrations (~100 µM). Acts synergistically with Imatinib (Cat. No. 504595) to reduce the proliferation of chronic myeloid leukemia (CML) cells.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532336
          Brand Family Calbiochem®
          Synonyms3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine, 2-((3-Benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)thio)oxazole, NADPH Oxidase Inhibitor VIII, VAS-3947
          References
          ReferencesSanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
          Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
          Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.
          Product Information
          FormLight yellow solid
          Hill FormulaC₁₄H₁₀N₆OS
          Chemical formulaC₁₄H₁₀N₆OS
          Applications
          Biological Information
          Primary TargetNADPH Oxidase
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          NOX Inhibitor VIII, VAS3947 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Sanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
          Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
          Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.

          Brochure

          Title
          NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
          New Products - Antibodies, Small Molecule, Inhibitors
          Pathways and Biomarkers of Oxidative Stress (EMD)

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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.

          Revision05-December-2014 JSW
          Synonyms3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine, 2-((3-Benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)thio)oxazole, NADPH Oxidase Inhibitor VIII, VAS-3947
          DescriptionA cell-permeable VAS2870 (Cat No. 492000) analogue that displays improved solubility and effectively blocks ROS production in DMSO-differentiated HL-60 cultures upon oxidative burst induction by PMA (IC50 = 1 µM by Cytochrome C reduction & 2 µM by L012 chemiluminescence; Drug added 30 min prior to 100 nM PMA/500582 & 524400) via NADPH oxidases/NOX inhibition, while displaying no potency against eNOS or xanthine oxidase/XOD enzymatic activity in cell-free assays even at a high concentration of 100 µM. Reported to suppress the high ROS level in isolated thoracis aortas sections from spontaneously hypertensive rats (SHRs) in situ (by 66% with 10 µM) and synergize with Imatinib (Cat. No. 504595) against the proliferation of p210 Bcr-abl-expressing murine Boff 210 cultures. A commonly employed NOX inhibitor Apocynin (Cat. No. 178385), in comparison, is shown to interfere with L012-based assays and exhibit little potency against NOX-mediated ROS production in DMSO-differentiated HL-60 cultures (by Cytochrome C reduction) or in cell-free assays using A7r5 & CaCo-2 homogenates (IC50 >1 mM), while another NOX inhibitor DPI (Cat. No. 300260) is shown to inhibit both eNOS & XOD activities.
          FormLight yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₄H₁₀N₆OS
          Purity≥98% 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesSanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
          Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
          Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.