AM-4668

Protein target name:

FFAR1

Mechanism of action:

Agonist

Recommended Concentration for use in cells:

up to 1 uM

Probe Availability

MedChemExpress

TOCRIS

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Free fatty acid receptor

HUGO ID:

HGNC:4508

Entrez gene ID:

2864

UNIPROT ID:

O14842

Target alias:

FFA1R, GPCR40, GPR40

Probe Details

Chemical Probes Portal ID:

CPP1764

Probe alias:

BDBM50019969, cpd 10

PubChem CID:

24897670

ChEMBL ID:

CHEMBL3287574

SMILES string:

CC1=C(SC(=N1)C2=CC=C(C=C2)C(F)(F)F)COC3=CC=C(C=C3)[C@H](CC(=O)O)C4=NOC=C4

InChi Key:

BMLGZNVPWRUVNM-IBGZPJMESA-N

Orthogonal probe:

FasiglifamTUG-469AMG-837

Physico-chemical properties

NMR:

1H NMR (500 MHz) (DMSO-d6) δ 8.76 (1H, s); 8.13 (2H, d, J=7Hz); 7.86 (2H, m); 7.26 (2H, d, J=6Hz); 7.01 (2H, m); 6.50 (1H, s); 5.23 (2H, s); 4.51 (1H, m); 3.20 (1H, m), 2.80 (1H, m), 2.47 (3H, s)

Validation in Cells and Model Organisms

In cell validation

On target activity in cells

Potency in cells:

EC50

36 nM aeq, 3.6 nM ip3

Potency assay (cells):

GPR40 aequorin assay, GPR40 IP3 assay

In vivo validation

Organism:

RatDogCyno

Dose:

0.5 mg/Kg IP, 2 mg/Kg PO

Route of delivery:

OralIntravenous

Plasma half life:

5.3 (R), 5.6 (D), 14 (C) h

Systemic clearance:

0.09 (R), 0.15 (D), 0.04 (C) L/h/Kg

Fraction of probe bound to plasma protein:

77 (R), 100 (D), 75 (C) %

Primary Reference

Reference (doi):

10.1021/ml400501x

Reference (PMID):

24900872

AM-4668

Probe Availability

Probe Information

Target Details

FFA1R, GPCR40, GPR40

Probe Details

Physico-chemical properties

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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AM-4668

Probe Availability

Probe Information

Target Details

FFA1R, GPCR40, GPR40

Probe Details

Physico-chemical properties

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?