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500487 Glucokinase Activator II - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₂FN₇O₃

Products

Catalog NumberPackaging Qty/Pack
5.00487.0001 Glass bottle 10 mg
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
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

Documentation

Glucokinase Activator II - Calbiochem 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 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.