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BIIE0246 | Antagonist of NPY2R
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
NPY2R
    • IC50:3.3 nM
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity vs family members was assessed on rat homologs using radioligand binding assay in HEK293 ...

    Potency
    Cellular
    In Vitro

    NPY2R

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/sj.bjp.0703162

    In Vivo Validations

    Mouse, Rat, Rabbit
    Dose: 3 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: <3h

    DOI Reference: 10.1038/sj.bjp.0703162

    Negative Control Compounds

    BIIE0212
    Notes: BIIE0212 is a congeneric analogue from the same series of L-argininamides with similar physicochemical properties but with a more than 400-fold lower affinity towards the Y2 receptor.

    Orthogonal Probes def

    JNJ-31020028
    ML075

    Chemical Information

    Molecular Formula C49H57N11O6
    SMILEs N=C(N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O
    InChI InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10,14-21,40,43H,11-13,22-33H2,(H,52,64)(H,54,61)(H,55,63)(H4,50,51,53)/t40-,43?/m0/s1
    Molecular weight 895.45 Da
    AlogP 3.4942700000000047
    HBond acceptors 17
    HBond donors 7
    Atoms 123

    Vendors

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    Expert Reviews

    by SERP
    (on 7 Jul 2021)
    Cellular Use Rating
    In Model Organisms
    For in vivo CNS studies inject intrathecally or directly in region of interest.
    by SERP+
    (on 14 Oct 2025)
    Cellular Use Rating
    In Model Organisms
    Consult opnME (Boehringer Ingelheim) for further in depth ADME and selectivity data. Due to the poor reported solubility, permeability, moderate metabolic stability (and PPB), BIIE0246 is not recommended...
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