VU6081679 |
VU6081679 : Positive Allosteric of GRM8
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| GRM8 |
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: selective over the other two widely CNS expressed Group III mGlus, ...
Selectivity Assessment Description:
Eurofins Lead Profiling Screen
Radioligand binding panel of 44 targets including GPCRs, ion channel ...
Potency Cellular
In Vitro
GRM8
Mode of Action: Positive Allosteric
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acschemneuro.6c00364
In Vivo Validations
Rat
Dose: 1 mg/Kg IV, 10 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
0.91 h
Systemic clearance:
22.4 mL/min/kg
Bioavailability:
102%
Volume of Distribution at Steady-State:
1.38 L/Kg
Target engagement assay:
Kp brain/plasma 0.16, Kp,uu brain/plasma 0.19
DOI Reference: 10.1021/acschemneuro.6c00364
Chemical Information
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