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ML075 | ML075 : peptide competitive 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
    • IC50:199 nM
    • Ki:Ki : 1.55 nM
    peptide competitive
    up to 1 µM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within target family: selective over Y1R, IC50 >35 uM Selectivity outside target family: ...

    Potency
    Cellular
    In Vitro

    NPY2R

    Mode of Action: peptide competitive

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1124/mol.109.058677

    In Vivo Validations

    Rat
    Dose: 10 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 62.4 min (serum), 438.1 min (hippocampus)
    Systemic clearance: 0.117 L/min/Kg (serum)
    Cmax: 2.90 uM (serum), 0.49 uM (hippocampus)
    Tmax: 15 min (serum), 30 min (hippocampus)
    Area Under the Curve:: 191.41 uM*min (serum), 94.95 uM*min (hippocampus)
    Volume of Distribution at Steady-State: 6.82 L/Kg (serum)

    DOI Reference: 10.1021/acschemneuro.9b00082

    Chemical Information

    Molecular Formula C27H30N2O2S
    SMILEs CCOc1ccc(NC(=S)N2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1
    InChI InChI=1S/C27H30N2O2S/c1-2-31-25-15-13-24(14-16-25)28-26(32)29-19-17-23(18-20-29)27(30,21-9-5-3-6-10-21)22-11-7-4-8-12-22/h3-16,23,30H,2,17-20H2,1H3,(H,28,32)
    Molecular weight 446.20 Da
    AlogP 0.0
    HBond acceptors 4
    HBond donors 2
    Atoms 62

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    Expert Reviews

    by SERP
    (on 2 Feb 2023)
    Cellular Use Rating
    In Model Organisms
    The maximum inhibitory effect of this compound looks like 80% or around based on the literature, the users may need to take into account this point.
    by SERP
    (on 14 Oct 2025)
    Cellular Use Rating
    In Model Organisms
    In cells the compound shows an IC50>100 nM and is selective in a panel of 40 different receptors, ion channels, and transporters found in the CNS. The compound contains some PAINS feature, however the...
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