371721

GPR40 Agonist II

The GPR40 Agonist II controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.

• Synonym(s): GPR40 Agonist II, 3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II, 3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid
• Empirical Formula (Hill Notation): C₁₆H₁₁Cl₂NO₂
• CAS Number: 1206629-08-4
• Molecular Weight: 320.17
• MDL number: MFCD30290778
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL, clear, colorless
• shipped in: wet ice
• storage temp.: 2-8°C
• SMILES string: ClC1=NC(Cl)=CC(C#CC2=CC=C(CCC(O)=O)C=C2)=C1

Description

General 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.

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C>

Other Notes

Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable