HG-10-102-01 |
HG-10-102-01 : Inhibitor of LRRK2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| LRRK2 (Mutant:WT, G2019S, A2016T, G2019S-A2016T) |
|
|
Inhibitor
up to 1 µM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The kinase selectivity of was assessed using standard radioactivity-based enzymatic assays against a ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
KiNativ approach to monitoring kinase inhibition in tissues from the inhibitor-treated animals. Of t ...
Potency Cellular
In Vitro
LRRK2
(Mutant:WT, G2019S, A2016T, G2019S-A2016T)
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/ml300123a
In Vivo Validations
Mouse
Dose: 10 mg/kg
Route of delivery:
Oral
Cmax:
806.27 ng/mL
Tmax:
0.25 h
Area Under the Curve::
502.34 h*ng/mL
Bioavailability:
67 %
DOI Reference: 10.1021/ml300123a
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.13 h
Systemic clearance:
222.04 mL/min/Kg
Cmax:
539.84 ng/mL
Area Under the Curve::
74.85 h*ng/mL
Volume of Distribution at Steady-State:
1.68 L/Kg
DOI Reference: 10.1021/ml300123a
Dose: 3, 10, 30, 50, and 100 mg/kg
Route of delivery:
Intraperitoneal
DOI Reference: 10.1021/ml300123a
Chemical Information
| Molecular Formula | C17H20ClN5O3 |
| SMILEs | CNc1nc(Nc2ccc(C(=O)N3CCOCC3)cc2OC)ncc1Cl |
| InChI | InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22) |
| Molecular weight | 377.13 Da |
| AlogP | 2.3963 |
| HBond acceptors | 8 |
| HBond donors | 2 |
| Atoms | 46 |