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T-10430 | T-10430 : Agonist of LTB4R2
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
LTB4R2
    • EC50:19 nM
    • EC50:0.51 nM
    • EC50:31 nM
    Agonist
    300-500 nM
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    The GPCR screen (314 receptors, Ca2+ Aequorin assay) shows no activity at 1 µM except for LTB4R2.
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Off-target test on BLT1 with T-10430 tested as agonist and off-target test on AT1 tested as antagoni ...

    Potency
    Cellular
    In Vitro

    LTB4R2

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.4c01617

    In Vivo Validations

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Subcutaneous
    Plasma half life: 62 min
    Cmax: 9120 ng/mL
    Tmax: 15 min
    Area Under the Curve:: 245000 ng*min/mL

    DOI Reference: 10.1021/acs.jmedchem.4c01617

    Dose: 3 mg/kg
    Route of delivery: Intravenous
    Plasma half life: 19 min
    Cmax: 3290 ng/mg
    Area Under the Curve:: 61100 ng*min/mL
    Bioavailability: 51%

    DOI Reference: 10.1021/acs.jmedchem.4c01617

    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 154 min
    Cmax: 1990 ng/mL
    Tmax: 15 min
    Area Under the Curve:: 104000 ng*min/mL

    DOI Reference: 10.1021/acs.jmedchem.4c01617

    Negative Control Compounds

    T-10430-NC
    Notes: Inactive at BLT2 (IP-One) up to 100 μM, EC50 (BLT2 cAMP) = 560 nM, 1000-fold higher EC50 in cAMP assay.

    Chemical Information

    Molecular Formula C17H22N6O
    SMILEs CCCCC(=O)N1CC2(C1)CN(c1ccccc1-c1nnn[nH]1)C2
    InChI InChI=1S/C17H22N6O/c1-2-3-8-15(24)23-11-17(12-23)9-22(10-17)14-7-5-4-6-13(14)16-18-20-21-19-16/h4-7H,2-3,8-12H2,1H3,(H,18,19,20,21)
    Molecular weight 326.19 Da
    AlogP 1.7055
    HBond acceptors 7
    HBond donors 1
    Atoms 46

    Expert Reviews

    by SERP
    (on 1 Feb 2025)
    Cellular Use Rating
    In Model Organisms
    Although one may use this compound for in vitro studies with a general experimental procedure, users should have full awareness of potential limitations of this compound for in vivo studies due to its...
    by SERP
    (on 22 Feb 2025)
    Cellular Use Rating
    In Model Organisms
    At the cellular level, the compound exhibits satisfactory selectivity; however, its potency is suboptimal. The current working concentration of 100 nM may be insufficient, and an increase is recommended....
    by SERP
    (on 8 Jan 2026)
    Cellular Use Rating
    In Model Organisms
    There are useful links in the PubChem compound entry below for T-10430, compound 20 in the patent and the paper https://pubchem.ncbi.nlm.nih.gov/compound/172676849 This includes three vendor links but...
    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