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VU6081679 | VU6081679 : Positive Allosteric of GRM8
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GRM8
    • EC50:162 nM
    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

    Coming Soon...

    References

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    Cross References

    Expert Reviews

    No SERP comments found for VU6081679

    Probe VU6081679 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.