GPR120-IN-1

Protein target name:

FFAR4

Mechanism of action:

Agonist

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:

HGNC:19061

Entrez gene ID:

338557

UNIPROT ID:

Q5NUL3

Target alias:

BMIQ10, GPR120, GPR129, GT01, O3FAR1, PGR4

Probe Details

Chemical Probes Portal ID:

CPP2190

Probe alias:

cpdA

PubChem CID:

73777063

ChEMBL ID:

CHEMBL3919973

SMILES string:

O=C(O)CC(CC1)CCC21CCN(C3=CC(OC(F)(F)F)=CC=C3Cl)CC2

InChi Key:

WUJVPELCYCESAP-UHFFFAOYSA-N

Orthogonal probe:

TUG-891

Validation in Cells and Model Organisms

In cell validation

On target activity in cells

Potency in cells:

pEC50

7.6

Potency assay (cells):

Fluorometric calcium assay using FLIPR methodology

Off target activity in cells

Probe Selectivity in Cell:

No activity detected on FFAR1 in both human and mouse variants.

In vivo validation

Organism:

Mouse

Dose:

30 mg/Kg

Primary Reference

Reference (doi):

10.1038/nm.3614

Reference (PMID):

24997608

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB Comments

This probe (cpdA) was demonstrated to show excellent cellular activity on and submicromolar activity in a cellular beta-arrestin interaction assay in GPR120-transfected cells. In vivo, the probe was found to exhibit beneficial metabolic effects in a standard high fat-fed obese mouse model, including anti-inflammatory effects on macrophages both in vitro and in vivo, improved glucose tolerance, and increased insulin sensitivity. The fact that the probe completely lacked Ca++ mobilization activity in a GPR40 (FFAR1) overexpressing cell line, and did not have appreciable in vivo metabolic effects in a GPR120 knockout mouse provides strong evidence that the published phenotypic effects of cpdA are due to on-target agonistic activity of GPR120. Moreover, because this compound has a highly drug-like scaffold and has in vivo activity through PO administration, it is, therefore, a valuable and recommended probe to use in a variety of settings. No biochemical binding data has been published for this probe, likely because of the challenges in developing the relevant assays for this target class. Because its activity against other target classes has not been published, additional confirmatory studies for cpdA are likely necessary to conclusively prove on-mechanism activity in other applications. Finally, because no pharmacokinetic data have been published for cpdA, care must be taken when adjusting doses in mice or when dosing in other species (e.g. diabetic or obese rats).

Jul 26 2021 - 11:58am

There is insufficient off-target data on the compound and no raw data were supplied to assess the efficacy and potency of the compound of interest. Without a negative control as well as comprehensive off-target profiling it is not recommended using this probe.

Aug 5 2021 - 8:59am

Up to 500 micromoles/L of GPR120-IN-1 can be applied topically to the mouse tongue to stimulate fatty acid taste reception; Yasumatsu et al. (doi:10.111/apha.13215) have established, using GPR120 knockout mice, that such application of GPR120-IN-1 to the mouse tongue can elicit chorda tympani nerve responses only in wildtype mice, thereby independently establishing the target of GPR120-IN-1 as GPR120.

Sep 30 2021 - 10:12am

GPR120-IN-1

Probe Availability

Probe Information

Target Details

BMIQ10, GPR120, GPR129, GT01, O3FAR1, PGR4

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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GPR120-IN-1

Probe Availability

Probe Information

Target Details

BMIQ10, GPR120, GPR129, GT01, O3FAR1, PGR4

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?