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371721

Sigma-Aldrich

GPR40 Agonist II

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

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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
Molecular Weight:
320.17
MDL number:

Quality Level

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

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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