PF-06471553 |
PF-06471553 : Inhibitor of MOGAT3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MOGAT3 |
|
|
Inhibitor
up to 10 uM
Selectivity
In Vitro Selectivity Assessment
Selectivity Assessment Description:
PF-06471553 @ 10 μM was selective against a broad panel of more than 120 individual targets, includi ...
Potency Cellular
In Vitro
MOGAT3
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5b01008
In Vivo Validations
Mouse
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.4 h
Systemic clearance:
1.4 mL/min/kg
Volume of Distribution at Steady-State:
0.17 L/kg
DOI Reference: 10.1021/acs.jmedchem.5b01008
Dose: 5 mg/kg
Route of delivery:
Oral
Cmax:
9.3 μg/mL
Area Under the Curve::
27 μg·h/mL
Bioavailability:
74%
DOI Reference: 10.1021/acs.jmedchem.5b01008
Negative Control Compounds
Chemical Information
| Molecular Formula | C23H25N5O4S |
| SMILEs | COc1cccc(CC(=O)N2Cc3ccc(S(=O)(=O)Nc4cnn(C5CCC5)n4)cc3C2)c1 |
| InChI | InChI=1S/C23H25N5O4S/c1-32-20-7-2-4-16(10-20)11-23(29)27-14-17-8-9-21(12-18(17)15-27)33(30,31)26-22-13-24-28(25-22)19-5-3-6-19/h2,4,7-10,12-13,19H,3,5-6,11,14-15H2,1H3,(H,25,26) |
| Molecular weight | 467.16 Da |
| AlogP | 0.0 |
| HBond acceptors | 9 |
| HBond donors | 1 |
| Atoms | 58 |
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