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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

    Vendors

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    Expert Reviews

    by SERP
    (on 7 Nov 2023)
    Cellular Use Rating
    In Model Organisms
    (The reviewer did not leave any public 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