GPR40 Agonist II - Calbiochem (C15-1303-084)

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

Molecular Weight: 320.17. Empirical Formula: C₁₆H₁₁Cl₂NO₂. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.