Chemical Probes logo
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
Download

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

    canSAR7402268
    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