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481417 CRAC Channel Inhibitor IV, EVP4593 - Calbiochem

481417
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₂₀N₄O

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481417-5MG
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      Description
      OverviewA cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-κB activation in Jurkat cells (IC50 = 11 nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1 mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300 nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30 nM to 3 µM, which is consistent with TRPC1 knockdown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100 µM to 400 µM.
      Catalogue Number481417
      Brand Family Calbiochem®
      SynonymsN4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
      References
      ReferencesWu, J., et al. 2011. Chem Biol. 18, 777.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 383.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 3869.
      Product Information
      FormYellow powder
      Hill FormulaC₂₂H₂₀N₄O
      Chemical formulaC₂₂H₂₀N₄O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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 Regulatory Review
      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

      CRAC Channel Inhibitor IV, EVP4593 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      CRAC Channel Inhibitor IV, EVP4593 - Calbiochem Certificates of Analysis

      TitleLot Number
      481417

      References

      Reference overview
      Wu, J., et al. 2011. Chem Biol. 18, 777.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 383.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 3869.
      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.

      Revision19-February-2013 JSW
      SynonymsN4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
      DescriptionA cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-κB activation in Jurkat cells (IC50 = 11 nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1 mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300 nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30 nM to 3 µM, which is consistent with TRPC1 knockdown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100 µM to 400 µM.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₀N₄O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml; clear, yellow solution)
      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 Regulatory Review
      ReferencesWu, J., et al. 2011. Chem Biol. 18, 777.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 383.
      Tobe, M., et al. 2003. Bioorg. Med. Chem. 11, 3869.