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347423 β-Glucuronidase Inhibitor - CAS 484006-66-8 - Calbiochem

The β-Glucuronidase Inhibitor controls the biological activity of β-Glucuronidase.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea

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347423
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Tableau de caractéristiques principal

CAS #Empirical Formula
484006-66-8C₂₃H₂₇N₃O₃S

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347423-10MG
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      Description
      OverviewAn orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC50 = 283 nM; kcat/Km = 0.0987 s-1µM-1; Ki = 164 nM in vitro assays against E coli β-glucuronidase; EC50 = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>> 100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).
      Catalogue Number347423
      Brand Family Calbiochem®
      Synonyms1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
      References
      ReferencesWallace, B.D., et al. 2010. Science 330, 831.
      Product Information
      CAS number484006-66-8
      FormWhite solid
      Hill FormulaC₂₃H₂₇N₃O₃S
      Chemical formulaC₂₃H₂₇N₃O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥99% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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
      Global Trade Item Number
      Référence GTIN
      347423-10MG 04055977193183

      Documentation

      β-Glucuronidase Inhibitor - CAS 484006-66-8 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      β-Glucuronidase Inhibitor - CAS 484006-66-8 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      347423

      Références bibliographiques

      Aperçu de la référence bibliographique
      Wallace, B.D., et al. 2010. Science 330, 831.
      Fiche technique

      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.

      Revision10-August-2012 JSW
      Synonyms1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
      DescriptionAn orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC50 = 283 nM; kcat/Km = 0.0987 s-1µM-1; Ki = 164 nM in vitro assays against E coli β-glucuronidase; EC50 = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>> 100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number484006-66-8
      Chemical formulaC₂₃H₂₇N₃O₃S
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesWallace, B.D., et al. 2010. Science 330, 831.