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509665 Glucokinase Activator III, Ro-28-1675 - CAS 300353-13-3 - Calbiochem

A cell-permeable activator of glucokinase. Exhibits in vivo glucose-lowering and insulin-releasing activity

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Synonymes: GK Activator III, Hexokinase D Activator III, Hexokinase IV Activator III, Ro-28-0450 (R)-enantiomer, RO0281675

Primary Target: Glucokinase
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509665
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Tableau de caractéristiques principal

CAS #Empirical Formula
300353-13-3C₁₈H₂₂N₂O₃S₂

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      Description
      OverviewA cell-permeable thiazolyl-propanamide compound that acts as a glucokinase (GK) activator by increasing Vmax and decreasing [S]1/2 of GK-catalyzed reaction as well as freeing GK from the inhibitory action of GK regulatory protein (GKRP), resulting in increased. Induces GK nuclear-to-cytosol translocation in primary rat hepatocytes and reduces glucose concentration for insulin secretion stimulation from isolated rat pancreatic islets (threshold [glucose] = 3 mM vs 6 mM with or without 3 µM Ro-28-1675). Exhibits in vivo glucose-lowering and insulin-releasing activity in non-diabetic C57BL/6 mice and Wistar rats and is efficacious in several murine and rodent type II diabetes mellitus (T2DM) models (10 to 50 mg/kg via p.o.). Does not affect hexokinase I or II activity.
      Catalogue Number509665
      Brand Family Calbiochem®
      SynonymsGK Activator III, Hexokinase D Activator III, Hexokinase IV Activator III, Ro-28-0450 (R)-enantiomer, RO0281675
      References
      ReferencesWolff, M., et al. 2008. J. Biomol. Screen 13, 837.
      Grimsby, J., et al. 2003. Science 301, 370.
      Product Information
      CAS number300353-13-3
      FormWhite powder
      Hill FormulaC₁₈H₂₂N₂O₃S₂
      Chemical formulaC₁₈H₂₂N₂O₃S₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGlucokinase
      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
      Global Trade Item Number
      Référence GTIN
      5.09665.0001 04055977241013

      Documentation

      Glucokinase Activator III, Ro-28-1675 - CAS 300353-13-3 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Wolff, M., et al. 2008. J. Biomol. Screen 13, 837.
      Grimsby, J., et al. 2003. Science 301, 370.
      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.

      Revision28-April-2014 JSW
      SynonymsGK Activator III, Hexokinase D Activator III, Hexokinase IV Activator III, Ro-28-0450 (R)-enantiomer, RO0281675
      DescriptionA cell-permeable thiazolyl-propanamide compound that acts as an allosteric glucokinase-(GK) selective activator, increasing Vmax and decreasing [S]1/2 (by 1.5- and 4.3-fold, respectively, at 3 µM; [Glucose] = 5 mM) in human GK enzymatic assays, as well as freeing GK from the inhibitory action of GK regulatory protein (GKRP), resulting in increased GK nuclear-to-cytosol translocation in primary rat hepatocytes (EC50/[Glucose] = 0.16 µM/16.8 mM, 0.27 µM/8.4 mM, 2.2 µM/2.8 mM) and reduced glucose concentration for stimulating insulin secretion from isolated rat pancreatic islets (threshold [glucose] = 3 mM vs 6 mM with or without 3 µM Ro-28-1675). Exhibits in vivo glucose-lowering and insulin-releasing activity in non-diabetic C57BL/6 mice and Wistar rats and is efficacious in several murine (KK/Upj-Ay/J, ob/ob, and diet-induced obese C57BL/6) and rodent (Goto-Kakizaki) type II diabetes mellitus (T2DM) models (10 to 50 mg/kg via p.o.), while efficacy is no longer observed in older hypoinsulinemic db/db mice with blood glucose levels reaching 300 mg/dl. Reported not to affect the activity of hexokinase I or II and display no activity toward GK-independent insulin release from β cells upon 2-Ketoisocaproic acid (α-KIC) stimulation.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number300353-13-3
      Chemical formulaC₁₈H₂₂N₂O₃S₂
      Purity≥98% by HPLC
      SolubilityDMSO (100 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
      ReferencesWolff, M., et al. 2008. J. Biomol. Screen 13, 837.
      Grimsby, J., et al. 2003. Science 301, 370.