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500487 Glucokinase Activator II - CAS 1245214-64-5 - Calbiochem

A cell-permeable compound that reduces glucokinase Km for glucose (EC₅₀ = 120 nM & 350 nM, for human and rat enzyme). Enhances insulin secretion from INS-1 cells upon glucose exposure.

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Synonyme: 4-((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

Primary Target: Glucokinase
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500487
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1245214-64-5C₂₄H₂₂FN₇O₃

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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
      CAS number1245214-64-5
      FormOff-white solid
      Hill FormulaC₂₄H₂₂FN₇O₃
      Chemical formulaC₂₄H₂₂FN₇O₃
      ReversibleY
      Quality LevelMQ100
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5004870001 04055977245561

      Documentation

      Glucokinase Activator II - CAS 1245214-64-5 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Pfefferkorn, J. A., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7100.
      Datenblatt

      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
      CAS number1245214-64-5
      Chemical formulaC₂₄H₂₂FN₇O₃
      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 (=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.