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VX548 | VX548 : Inhibitor of SCN10A
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
SCN10A
    • IC50:0.68 ± 0.16 nM
    Inhibitor
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    In a panel of recombinant NaV1.1 to NaV1.9 VX548 showed exquisite selectivity for NaV1.8 with at lea ...
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Suzetrigine is broadly selective against 180 targets in vitro, including 44 targets associated with ...

    Potency
    Cellular
    In Vitro

    SCN10A

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1056/NEJMoa2209870

    In Vivo Validations

    Rat
    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 3.7 (F), 1.9 (M) h
    Systemic clearance: 12.5 (F), 65.1 (M) mL/min/Kg
    Area Under the Curve:: 1505.8 (F), 253.8 (M) ng*h/mL
    Volume of Distribution at Steady-State: 5.0 (F), 7.2 (M) L/Kg

    DOI Reference: 10.1002/bdd.2387

    Dose: 2 mg/Kg
    Route of delivery: Oral
    Plasma half life: 4.9 (F), 2.5 (M) h
    Cmax: 369.6 (F), 31.7 (M) ng/mL
    Tmax: 0.5–1 (F), 0.5–1 (M) h
    Area Under the Curve:: 2905.2 (F), 56.9 (M) ng*h/mL
    Bioavailability: 96 (F), 11 (M) %

    DOI Reference: 10.1002/bdd.2387

    Chemical Information

    Molecular Formula C21H20F5N3O4
    SMILEs COc1c([C@H]2[C@H](C(=O)Nc3ccnc(C(N)=O)c3)O[C@@](C)(C(F)(F)F)[C@H]2C)ccc(F)c1F
    InChI InChI=1S/C21H20F5N3O4/c1-9-14(11-4-5-12(22)15(23)16(11)32-3)17(33-20(9,2)21(24,25)26)19(31)29-10-6-7-28-13(8-10)18(27)30/h4-9,14,17H,1-3H3,(H2,27,30)(H,28,29,31)/t9-,14-,17+,20+/m0/s1
    Molecular weight 473.14 Da
    AlogP 0.0
    HBond acceptors 7
    HBond donors 3
    Atoms 53

    Vendors

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    Expert Reviews

    by SERP
    (on 30 May 2024 )
    Cellular Use Rating
    In Model Organisms
    VX-548 is suitable for human cell-based studies and PK studies in rats, but I could not find efficacy data or patch clamp data on VX-548 in rats as of May 2024. It is important to note the major PK differences...
    by SERP
    (on 3 Jun 2024 )
    Cellular Use Rating
    In Model Organisms
    This is a very good compound for Nav 1.8 ion channels with very good selectivity within target class, but no information is found of selectivity outside target family. Unfortunately, no negative control...
    by SERP
    (on 14 Jun 2024 )
    Cellular Use Rating
    In Model Organisms
    The high selectivity and potency of VX-548 make it an ideal tool for studying the function of the NaV1.8 channel, notably for its physiological and pathological effects at the cellular level. VX-548 has...
    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