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508941 GPR40 Agonist III - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₁₅NO₂

Products

Catalog NumberPackaging Qty/Pack
5.08941.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number508941
Brand Family Calbiochem®
SynonymsFree Fatty Acid Receptor 1 Agonist III, FFA1 Agonist III
References
ReferencesChristiansen, E., et al. 2013. J. Med. Chem. 56, 982.
Product Information
FormOff-white powder
Hill FormulaC₁₉H₁₅NO₂
Chemical formulaC₁₉H₁₅NO₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
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 or with Dry 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 (-20°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
Catalog Number GTIN
5.08941.0001 04055977261448

Documentation

GPR40 Agonist III - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Christiansen, E., et al. 2013. J. Med. Chem. 56, 982.
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.

Revision07-March-2014 JSW
SynonymsFree Fatty Acid Receptor 1 Agonist III, FFA1 Agonist III
DescriptionA cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₉H₁₅NO₂
Structure formulaStructure formula
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 3 months at -20°C.
Toxicity Standard Handling
ReferencesChristiansen, E., et al. 2013. J. Med. Chem. 56, 982.