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BI-2081 | BI-2081 : Agonist of FFAR1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (2 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:23 nM
  • EC50:3-5 nM
Agonist
extracellular target
up to 200 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Eurofins Safety Panel (44 GPCRs at 10 μM): Closest off-targets (Kd [µM]): ADRA2C (0.840), ADRA2A (1. ...

Potency
Cellular
In Vitro

FFAR1

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

Other Reference: Peer reviewed at SGC

In Vivo Validations

Rat
Dose: 1 mg/Kg IV, 10 mg/Kg PO
Route of delivery: Intravenous, Oral
Systemic clearance: 6.9% QH
Tmax: 1.17 h
Bioavailability: 79%
Volume of Distribution at Steady-State: 0.9 L/Kg

Other Reference: Peer reviewed at SGC

Negative Control Compounds

CANSAR3894697
Notes: BI-0340: EC50 = 1230 nM (human IPOne assay); Eurofins Safety Panel 44™: clean (closest off-target: NR3C1 (57 % inh. at 10 µM))

Orthogonal Probes def

CANSAR735732

Chemical Information

Molecular Formula C32H35FO6
SMILEs Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O
InChI InChI=1S/C32H35FO6/c1-18-13-22(37-12-11-32(3,4)36)14-19(2)30(18)24-7-9-26(33)31-25(24)8-10-27(31)39-21-5-6-23-20(15-29(34)35)17-38-28(23)16-21/h5-7,9,13-14,16,20,27,36H,8,10-12,15,17H2,1-4H3,(H,34,35)/t20-,27-/m1/s1
Molecular weight 534.24 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 74

Expert Reviews

by SERP
(on 19 Feb 2024)
In Model Organisms
(The reviewer did not leave any public comments)
by SERP+
(on 14 Oct 2025)
Cellular Use Rating
In Model Organisms
This is a well validated for in cell probe use. The in vivo data lack demonstration of target engagement, but PK properties reported and favorable.
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