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MAVATREP | Antagonist of TRPV1
RATINGS:
Cellular Use: (0 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TRPV1
    • IC 50:7 nM
    • IC 50:4.6 nM
    Antagonist
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    In cytochrome P450 isoenzyme studies in human liver microsomes, Mavatrep exhibited minimal effect on ...

    Potency
    Cellular
    In Vitro

    TRPV1

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    In Vivo Validations

    Rat
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 3.8 h
    Cmax: 421 ng/mL
    Area Under the Curve:: 4203 ng*h/mL
    Bioavailability: 51 %

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 3.4 h
    Systemic clearance: 33 mL/min/kg
    Volume of Distribution at Steady-State: 10 L/kg

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 5.87 h
    Cmax: 944 ng/mL
    Bioavailability: 83.3 %
    Volume of Distribution at Steady-State: 13178 ng*h/mL

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 2.75 h
    Systemic clearance: 10.5 mL/min/kg
    Volume of Distribution at Steady-State: 2.5 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Dog
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 1.4 h
    Cmax: 1607 ng/mL
    Area Under the Curve:: 4186 ng*h/mL
    Bioavailability: 25 %

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.1 h
    Systemic clearance: 29 mL/min/kg
    Cmax: 969 ng/mL
    Volume of Distribution at Steady-State: 2.7 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Monkey (Rheus)
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 12.9 h
    Area Under the Curve:: 13747 ng*h/mL
    Bioavailability: 70 %

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 12.9 h
    Systemic clearance: 7 mL/min/kg
    Volume of Distribution at Steady-State: 3.8 L/kg

    DOI Reference: 10.1021/acs.jmedchem.5b00132

    Negative Control Compounds

    Cpd 28
    InChI: InChI=1S/C27H27N3O/c1-18(31)28-23-8-6-5-7-22(23)20-12-15-24-25(17-20)30-26(29-24)16-11-19-9-13-21(14-10-19)27(2,3)4/h5-17H,1-4H3,(H,28,31)(H,29,30)/b16-11+

    Orthogonal Probes def

    AM-404
    CAPSAICIN

    Chemical Information

    Molecular Formula C25H21F3N2O
    SMILEs CC(C)(O)c1ccccc1-c1ccc2[nH]c(/C=C/c3ccc(C(F)(F)F)cc3)nc2c1
    InChI InChI=1S/C25H21F3N2O/c1-24(2,31)20-6-4-3-5-19(20)17-10-13-21-22(15-17)30-23(29-21)14-9-16-7-11-18(12-8-16)25(26,27)28/h3-15,31H,1-2H3,(H,29,30)/b14-9+
    Molecular weight 422.16 Da
    AlogP 0.0
    HBond acceptors 3
    HBond donors 2
    Atoms 52

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    No SERP comments found for MAVATREP

    Probe MAVATREP is in the process of SERP review.

    Please continue to check back for new reviews and commentary.