AM-5262 |
Agonist of FFAR1
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 |
|
Agonist
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Panel screen data against 101 receptors: CEREP
Selectivity Assessment Description:
% of inhibition higher than 70% for 5/101:
A3R_Human 97%; TXA2 synthetase_Human 88%; COX2_ACE 85%; C ...
Potency Cellular
In Vitro
FFAR1
Mode of Action: Agonist
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/ml300427u
In Vivo Validations
Rat
Dose: 0.5 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
4.2 h
Systemic clearance:
0.25 L/h/kg
Volume of Distribution at Steady-State:
0.7 L/kg
DOI Reference: 10.1021/ml300427u
Monkey (Cynomolgus)
Dose: 0.5 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
2.2 h
Systemic clearance:
0.84 L/h/kg
Volume of Distribution at Steady-State:
1.4 L/Kg
DOI Reference: 10.1021/ml300427u
Chemical Information
| Molecular Formula | C33H35FO4 |
| SMILEs | COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 |
| InChI | InChI=1S/C33H35FO4/c1-32(2)13-4-5-27(32)25-15-20(6-10-24(25)26-16-22(37-3)9-11-30(26)34)19-38-23-8-7-21-12-14-33(28(21)17-23)18-29(33)31(35)36/h6-11,15-17,27,29H,4-5,12-14,18-19H2,1-3H3,(H,35,36)/t27-,29-,33-/m0/s1 |
| Molecular weight | 514.25 Da |
| AlogP | 7.6625 |
| HBond acceptors | 4 |
| HBond donors | 1 |
| Atoms | 73 |