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371721
Sigma-AldrichGPR40 Agonist II - CAS 1206629-08-4 - Calbiochem
The GPR40 Agonist II controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.
More>>The GPR40 Agonist II controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC50 = 40.7 nM in inducing Ca2+ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical and metabolic stability.
Catalogue Number
371721
Brand Family
Calbiochem®
Synonyms
3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II
References
References
Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.
GPR40 Agonist II - CAS 1206629-08-4 - Calbiochem Certificates of Analysis
Title
Lot Number
371721
References
Reference overview
Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.
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.
Revision
24-September-2012 JSW
Synonyms
3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II
Description
A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC50 = 40.7 nM in inducing Ca2+ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical (0.1% degradation after 12 days in PBS at 37 °C) and metabolic (3% metabolization by human liver S9 stability test) stability.
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1206629-08-4
Chemical formula
C₁₆H₁₁Cl₂NO₂
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml; clear, colorless solution)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C>
Toxicity
Standard Handling
References
Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.