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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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: Glucokinase
509665
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
300353-13-3C₁₈H₂₂N₂O₃S₂

Products

Catalogue NumberPackaging Qty/Pack
5.09665.0001 Glass bottle 10 mg
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
Catalogue Number GTIN
5.09665.0001 04055977241013

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Wolff, M., et al. 2008. J. Biomol. Screen 13, 837.
Grimsby, J., et al. 2003. Science 301, 370.
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.

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.