GW1100

Protein target name:

FFAR1

Mechanism of action:

Selective antagonist

Recommended Concentration for use in cells:

up to 10 uM

Probe Availability

MedChemExpress

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Free fatty acid receptor

HUGO ID:

FFAR1

Entrez gene ID:

2864

UNIPROT ID:

O14842

Target alias:

FFA1R, GPCR40, GPR40

Probe Details

Chemical Probes Portal ID:

CPP1755

Probe alias:

GW-1100

PubChem CID:

11692123

SMILES string:

CCOC1=NC=C(C=N1)CC2=CN(C(=NC2=O)SCC3=CC=C(C=C3)F)C4=CC=C(C=C4)C(=O)OCC

InChi Key:

PTPNCCWOTBBVJR-UHFFFAOYSA-N

Orthogonal probe:

FasiglifamTUG-469AMG-837

Physico-chemical properties

NMR:

1H NMR (400MHz, CDCl3, 25 ºC) δ 1.40 (m, 6H), 3.67 (s, 2H), 4.39 (m, 6H), 6.95 (m, 3H), 7.26 (m, 2H), 7.37 (d, J = 8.4 Hz, 2H), 8.16 (d, J = 8.4 Hz, 2H), 8.45 (s, 2H)

Validation in Cells and Model Organisms

In vitro validation

Off target activity

Probe Selectivity in Vitro:

GW1100 had no effect on the GPR120‐mediated stimulation of intracellular Ca2+ release; is shown to be selective against 220 other GPCRs

Outside target family: Selective in a panel comprising 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ, with the exception of the oxytocin receptor, for which it acted as an antagonist with a pIC50 6.9

In cell validation

On target activity in cells

Potency in cells:

pIC50, Kb

5.99, 1 uM

Potency assay (cells):

intracellular Ca2+ release stimulated by GW9508 or linoleic acid, α-linolenic acid, palmitic acid and cis-5,8,11,14,17-eicosapentaenoic acid, GPR40 reporter assay, MIN6 glucose-stimulated insulin secretion assay Cell Lines used: HEK293 stably transfected to express the human macrophage scavenging receptor, HEK293 cells expressing exogenous GPR40, hGPR40-5 × Gal/Gal4-Elk1-luc+ CHO, MIN6

Off target activity in cells

Probe Selectivity in Cell:

GW1100 has no effect on the GPR120‐mediated stimulation of intracellular Ca2+ release. Outside target family: Shown to be at least 100‐fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ, with the exception of the oxytocin receptor, for which it acted as an antagonist with a pIC50 6.9

In vivo validation

Organism:

Mouse

Dose:

10 ug/Mouse

Other route of delivery:

Intracerebroventricular injection

Primary Reference

Reference (doi):

10.1038/sj.bjp.0706770 10.1371/journal.pone.0081563

Reference (PMID):

16702987 24349089

GW1100

Probe Availability

Probe Information

Target Details

FFA1R, GPCR40, GPR40

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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GW1100

Probe Availability

Probe Information

Target Details

FFA1R, GPCR40, GPR40

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?