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ERTUGLIFLOZIN | ERTUGLIFLOZIN : Inhibitor of SLC5A2
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
SLC5A2
    • IC50:0.927 ± 0.369 nM
    Inhibitor
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within target family: Selective against h-SGLT1 IC50 2050 (>2000 fold)

    Potency
    Cellular
    In Vitro

    SLC5A2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/jm200049r

    In Vivo Validations

    Rat
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 4.1 h
    Systemic clearance: 4.04 mL/min/Kg
    Volume of Distribution at Steady-State: 1.13 L/Kg

    DOI Reference: 10.1021/jm200049r

    Dose: 5.0 mg/Kg
    Route of delivery: Oral
    Cmax: 1.94 ± 0.185 μg/mL
    Tmax: 1.0 h
    Bioavailability: 69%

    DOI Reference: 10.1021/jm200049r

    Chemical Information

    Molecular Formula C22H25ClO7
    SMILEs CCOc1ccc(Cc2cc([C@]34OC[C@](CO)(O3)[C@@H](O)[C@H](O)[C@H]4O)ccc2Cl)cc1
    InChI InChI=1S/C22H25ClO7/c1-2-28-16-6-3-13(4-7-16)9-14-10-15(5-8-17(14)23)22-20(27)18(25)19(26)21(11-24,30-22)12-29-22/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3/t18-,19-,20+,21-,22-/m0/s1
    Molecular weight 436.13 Da
    AlogP 1.3564999999999994
    HBond acceptors 7
    HBond donors 4
    Atoms 55

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    Expert Reviews

    by SERP
    (on 7 Nov 2023 )
    Cellular Use Rating
    In Model Organisms
    As a selective inhibitor, ERTUGLIFLOZIN exhibits excellent potency and selectivity in vitro, and good pharmacokinetics in vivo. However, it should be noted that information regarding off-target is still...
    by SERP
    (on 30 Dec 2023 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    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