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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C16H11Cl2NO2
CAS Number:
Molecular Weight:
320.17
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
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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

InChI

1S/C16H11Cl2NO2/c17-14-9-13(10-15(18)19-14)6-5-11-1-3-12(4-2-11)7-8-16(20)21/h1-4,9-10H,7-8H2,(H,20,21)

InChI key

GCWBKYDSSJIRNJ-UHFFFAOYSA-N

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.

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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