Chemical Probes logo
ONO-8430506 | ONO-8430506 : Inhibitor of ENPP2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ENPP2
  • IC50:5.1 nM
  • IC50:4.5 nM
  • IC50:20-30 nM
    Inhibitor
    NA

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    ONO-8430506 was proved to be a selective inhibitor of ATX/ENPP2 as the compound showed no inhibition ...

    Potency
    Cellular
    In Vitro

    ENPP2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1371/journal.pone.0093230

    In Vivo Validations

    Rat
    Dose: 0.3 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 3.4 ± 0.9 h
    Systemic clearance: 8.19 ± 2.31 mL/min/Kg
    Area Under the Curve:: 0.647 ± 0.192 ug*h/mL
    Volume of Distribution at Steady-State: 1480 ± 150 mL/Kg

    DOI Reference: 10.1371/journal.pone.0093230

    Dose: 1 mg/Kg
    Route of delivery: Oral
    Plasma half life: 2.5 ±0.3 h
    Cmax: 0.261 ± 0.107 ug/mL
    Tmax: 1.2 ± 0.8 h
    Area Under the Curve:: 1.11 ± 0.27 ug*h/mL
    Bioavailability: 51.5%

    DOI Reference: 10.1371/journal.pone.0093230

    Mouse
    Dose: 1 mg/Kg
    Route of delivery: Oral
    Plasma half life: 5.4 ± 2.1 h
    Cmax: 124 ± 49 ng/mL

    DOI Reference: 10.1021/acsmedchemlett.0c00200

    Dog
    Dose: 0.3 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 8.9 ± 5.3 h
    Systemic clearance: 4.7 ± 0.7 mL/min/Kg
    Volume of Distribution at Steady-State: 1863 ± 878 mL/Kg

    DOI Reference: 10.1021/acsmedchemlett.0c00200

    Dose: 1 mg/Kg
    Route of delivery: Oral
    Plasma half life: 5.9 ± 2.0 h
    Cmax: 1670 ± 610 ng/mL
    Bioavailability: 71.1%

    DOI Reference: 10.1021/acsmedchemlett.0c00200

    Monkey (Cynomolgus)
    Dose: 0.3 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 7.9 ± 1.0 h
    Systemic clearance: 5.8 ± 0.6 mL/min/Kg
    Volume of Distribution at Steady-State: 2275 ± 235 mL/Kg

    DOI Reference: 10.1021/acsmedchemlett.0c00200

    Dose: 1 mg/Kg
    Route of delivery: Oral
    Cmax: 63 ± 38 ng/mL
    Bioavailability: 30.8%

    DOI Reference: 10.1021/acsmedchemlett.0c00200

    Chemical Information

    Molecular Formula C27H28FN3O3
    InChI InChI=1S/C27H28FN3O3/c28-19-5-3-18(4-6-19)15-31-22-16-30(13-7-20(22)21-2-1-12-29-24(21)31)23(32)14-26-8-10-27(17-26,11-9-26)25(33)34/h1-6,12H,7-11,13-17H2,(H,33,34)
    Molecular weight 461.21 Da
    AlogP 0.0
    HBond acceptors 6
    HBond donors 1
    Atoms 62

    Expert Reviews

    by SERP
    (on 16 Apr 2025 )
    In Model Organisms
    ONO-8430506 is a potent and selective inhibitor of ENPP2 (also known as Autotaxin, ATX). It shows robust PD activity in rat (inhibition of LPA formation in plasma), and regulates urethral tension in a...
    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