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AM-6226 | Full Agonist of FFAR1
RATINGS:
Cellular Use: (2 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
  • EC50:130 nM
  • IC50:5.7 nM
  • IC50:940 nM
Full Agonist
up to 10 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
AM-6226 did not activate the receptors GPR41 (FFAR3) and GPR43 (FFAR2) up to 10 µM, but had weak ...

Potency
Cellular
In Vitro

FFAR1

Mode of Action: Full Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acsmedchemlett.8b00213

In Vivo Validations

Rat
Dose: 0.5 mg/kg
Route of delivery: Intravenous
Plasma half life: 2 h

DOI Reference: 10.1021/acsmedchemlett.8b00213

Dose: 2 mg/Kg
Route of delivery: Oral
Systemic clearance: 0.33 L/h/kg
Cmax: 1.18 uM
Area Under the Curve:: 8.22 μM*h
Fb : >99%
Bioavailability: 72%
Volume of Distribution at Steady-State: 0.81 L/kg

DOI Reference: 10.1021/acsmedchemlett.8b00213

Dog
Dose: 0.5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 4.1 h

DOI Reference: 10.1021/acsmedchemlett.8b00213

Dose: 2 mg/Kg
Route of delivery: Oral
Systemic clearance: 0.21 L/h/kg
Area Under the Curve:: 11.6 μM*h
Fb : >99%
Bioavailability: 62 %
Volume of Distribution at Steady-State: 0.68 L/kg

DOI Reference: 10.1021/acsmedchemlett.8b00213

Monkey (Cynomolgus)
Dose: 0.5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.3 h

DOI Reference: 10.1021/acsmedchemlett.8b00213

Dose: 10 mg/Kg
Route of delivery: Oral
Systemic clearance: 0.22 L/h/kg
Area Under the Curve:: 80.4 μM*h
Fb : >99%
Bioavailability: 91 %
Volume of Distribution at Steady-State: 0.5 L/kg

DOI Reference: 10.1021/acsmedchemlett.8b00213

Orthogonal Probes def

GW1100
Fasiglifam
TUG-469

Chemical Information

Molecular Formula C32H36F2O4
SMILEs CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1F
InChI InChI=1S/C32H36F2O4/c1-5-21(17-30(35)36)23-8-6-10-29(31(23)34)38-19-20-11-13-24(26-18-22(37-4)12-14-28(26)33)25(16-20)27-9-7-15-32(27,2)3/h6,8,10-14,16,18,21,27H,5,7,9,15,17,19H2,1-4H3,(H,35,36)/t21-,27+/m1/s1
Molecular weight 522.26 Da
AlogP 8.4814
HBond acceptors 4
HBond donors 1
Atoms 74

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 22 Nov 2021 )
Cellular Use Rating
In Model Organisms
Although the authors provide off-target assessment within the family, off-target evaluation of other GPCRs, ion channels, transporters, kinases and similar are not provided. Without such information it...
by SERP
(on 24 Nov 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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