500487 Glucokinase Activator II - Calbiochem

500487
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₂₂FN₇O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00487.0001
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      Stocked 
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable indazole derivative that reduces glucokinase Km for glucose (EC50 = 120 nM and 350 nM, respectively, for human and rat enzyme) and effectively enhances insulin secretion from rat insulinima INS-1 cells upon 5 mM glucose exposure (EC50 = 170 nM). Shown to exhibit blood glucose lowering efficacy in OGTT (2 g/kg oral glucose challenge 1 h after single drug oral dosage) test among fasted rats (22% reduction of AUC; 250 mg/kg p.o.) in vivo.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number500487
          Brand Family Calbiochem®
          Synonyms4-((6-(azetidine-1-carbonyl)-5-fluoropyridin-3-yl)oxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide, Hexokinase IV Activator II, Hexokinase D Activator II, GK Activator II
          References
          ReferencesPfefferkorn, J. A., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7100.
          Product Information
          FormOff-white solid
          Hill FormulaC₂₄H₂₂FN₇O₃
          Chemical formulaC₂₄H₂₂FN₇O₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetGlucokinase
          Primary Target IC<sub>50</sub>EC₅₀ = 12 nM
          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 Shipped at Ambient Temperature or with Blue 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 (=2-°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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Pfefferkorn, J. A., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7100.
          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.

          Revision20-June-2014 JSW
          Synonyms4-((6-(azetidine-1-carbonyl)-5-fluoropyridin-3-yl)oxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide, Hexokinase IV Activator II, Hexokinase D Activator II, GK Activator II
          DescriptionA cell-permeable indazole derivative that reduces glucokinase Km for glucose (EC50 = 120 nM and 350 nM, respectively, for human and rat enzyme) and effectively enhances insulin secretion from rat insulinima INS-1 cells upon 5 mM glucose exposure (EC50 = 170 nM). Shown to be orally available in rats (F = 69%; Cmax = 1490 ng/mL; t1/2 = 2.6 hr; AUC = 5440 ng·hr/mL; 5 mg/kg p.o.) and exhibit blood glucose lowering efficacy in OGTT (2 g/kg oral glucose challenge 1 h after single drug oral dosage) test on fasted rats (22% reduction of AUC; 250 mg/kg p.o.) in vivo.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₄H₂₂FN₇O₃
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (=2-°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesPfefferkorn, J. A., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7100.