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Fasiglifam | Agonist of FFAR1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FFAR1
  • Ki:38 nM
  • Ki:140 nM
  • EC50:14 nM
Agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selective against FFAR2, FFAR3 (no activity up to 10uM)

Potency
Cellular
In Vitro

FFAR1

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/ml1000855

In Vivo Validations

Rat, Dog
Dose: 1 IV, 3 PO mg/Kg Rat, 0.5 IV, 1 PO mg/Kg Dog
Route of delivery: Intravenous, Oral
Plasma half life: 4.1 (R)-7.5 (D) h
Systemic clearance: 34.2 (R), 29.8 (D) mL/h/kg

DOI Reference: 10.1021/ml1000855

Negative Control Compounds

cpd 9b

Orthogonal Probes def

TUG-469
AMG-837

Chemical Information

Molecular Formula C29H32O7S
SMILEs Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
InChI InChI=1S/C29H32O7S/c1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24/h4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31)/t23-/m1/s1
Molecular weight 524.19 Da
AlogP 5.31364
HBond acceptors 7
HBond donors 1
Atoms 69

Vendors

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Expert Reviews

by SERP
(on 29 Mar 2021 )
Cellular Use Rating
In Model Organisms
Fasiglifam is an ago-allosteric modulator of free fatty acid receptor 1 (FFAR1(GPR40)), which amplifies the agonistic activity of the endogenous ligand c-linolenic acid (c-LA) by binding to an allosteric...
by SERP
(on 10 Apr 2021 )
Cellular Use Rating
In Model Organisms
Compound not tested for x-reactivity outside the FAR-family. The liver safety aspect has been mechanistically investigated in https://pubmed.ncbi.nlm.nih.gov/30243991/ and https://pubmed.ncbi.nlm.nih.gov/28206647/ Primary...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
This is a good probe for cellular use, however it has not been screened against a wider panel of related unrelated off-targets. Other reported GPR40 agonists have been more comprehensively screened against...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria