530656 LTA4 Epoxide Hydrolase Inhibitor, ARM1 - Calbiochem

530656
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₄N₂S

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      5.30656.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable benzylphenyl-thiazolamine compound that acts as a selective inhibitor against the epoxide hydrolase activity of leukotriene A4 hydrolase (LTA4H; Ki = 2.3 µM) and inhibits A23187- (Cat. Nos. 100105 & 100106) induced leukotriene B4 (LTB4) synthesis in primary human polymorphonuclear neutrophil (PMN) cultures (IC50 = 0.5 µM). Does not affect LTA4H aminopeptidase activity toward the cleavage of Pro-Gly-pro even at a high concentratin of 100 µM. Binds to the hydrophobic pocket that accommodates LTA4 ω-end, which is distant from the aminopeptidase active site.
          Catalogue Number530656
          Brand Family Calbiochem®
          Synonyms4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq, LTA4H Inhibitor
          References
          ReferencesStsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 4227.
          Product Information
          FormLight beige powder
          Hill FormulaC₁₆H₁₄N₂S
          Chemical formulaC₁₆H₁₄N₂S
          ReversibleY
          Applications
          Biological Information
          Primary TargetLTA4
          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

          LTA4 Epoxide Hydrolase Inhibitor, ARM1 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Stsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 4227.
          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.

          Revision04-June-2014 JSW
          Synonyms4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq, LTA4H Inhibitor
          DescriptionA cell-permeable benzylphenyl-thiazolamine compound that selectively inhibits against the leukotriene (LT) A4 epoxide hydrolase activity of LTA4H by occupying the same hydrophobic tunnel (Ki = 2.3 µM) targeted by LTA4 ω-end, displaying much reduced potency against LTA4H aminopeptidase activity (% inhibition/[ARM1] = 0/100 µM & 35/1 mM; Substrate = 800 µM Pro-Gly-Pro) coordinated by E296 and the catalytic site Zn2+ at the adjacent hydrophilic peptide substrate-binding cavity. Shown to inhibit A23187- (Cat. Nos. 100105 & 100106) induced LTB4 production in primary human polymorphonuclear neutrophil (PMN) cultures (IC50 = 0.5 µM; ARM1 added 10 min prior to 5 min stimulation by 2.5 µM A23187). Another LTA4H inhibitor SC 57461A (CAS 423169-68-0), in comparison, inhibits both the LTA4-to-LTB4 conversion as well as the chemotactic tripeptide Pro-Gly-Pro degradation activity of LTA4H.
          FormLight beige powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₄N₂S
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesStsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 4227.