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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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