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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      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®
      SynonymsLTA4H Inhibitor, 4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq
      References
      ReferencesStsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 4227.
      Product Information
      FormLight beige powder
      Hill FormulaC₁₆H₁₄N₂S
      Chemical formulaC₁₆H₁₄N₂S
      ReversibleY
      Quality LevelMQ100
      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
      SynonymsLTA4H Inhibitor, 4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq
      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.