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PF-3274167 | PF-3274167 : Antagonist of OXTR
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
OXTR
    • Ki:9.5 nM
    Antagonist
    300-500 nM
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selective against V1A Ki >1000 nM, V1B Ki >1000 nM, V2 Ki > 10000 nM. Profiled against a wide range ...

    Potency
    Cellular
    In Vitro

    OXTR

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.bmcl.2009.11.097

    In Vivo Validations

    Rat
    Dose: 2 mg/Kg
    Route of delivery: Oral
    Plasma half life: 0.9 h
    Systemic clearance: 36 mL/min/kg
    Bioavailability: 62%
    Volume of Distribution at Steady-State: 2.5 L/Kg

    DOI Reference: 10.1016/j.bmcl.2009.11.097

    Dog
    Dose: 0.2 mg/Kg
    Route of delivery: Oral
    Plasma half life: 1.9 h
    Systemic clearance: 8 mL/min/kg
    Bioavailability: 81%
    Volume of Distribution at Steady-State: 1.3 L/Kg

    DOI Reference: 10.1016/j.bmcl.2009.11.097

    Chemical Information

    Molecular Formula C19H19ClFN5O3
    SMILEs COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
    InChI InChI=1S/C19H19ClFN5O3/c1-27-11-17-23-24-19(26(17)13-4-6-18(28-2)22-8-13)25-9-14(10-25)29-16-5-3-12(21)7-15(16)20/h3-8,14H,9-11H2,1-2H3
    Molecular weight 419.12 Da
    AlogP 2.8774000000000006
    HBond acceptors 8
    HBond donors --
    Atoms 48

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    Expert Reviews

    by SERP
    (on 7 Nov 2023 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 23 Nov 2023 )
    Cellular Use Rating
    In Model Organisms
    As the Ki for the related off-target V1A is ~ 1µM, it is suggested to apply slightly lower maximum test concentration of 300-500 nM. PF- 3274167 has a Ki/Kd of 5-10 nM depending on different literature...
    by SERP
    (on 6 Dec 2023 )
    Cellular Use Rating
    In Model Organisms
    This compound https://pubchem.ncbi.nlm.nih.gov/compound/11683187 is rather old (in PubChem since 2006). It has also been designed as a drug by Pfizer not a probe and now has not only a code PF-3274167...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria