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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

Vendors

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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 public comments)
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