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TENAPANOR | TENAPANOR : Inhibitor of SLC9A3
RATINGS:
Cellular Use: (0 reviews)

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

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Targets Biochemical/Biophysical Potency Cellular Potency
SLC9A3
    • IC50:0.5 nM
    Inhibitor
    0.1-10 mg/kg in rats.. Statistically significant effects can be seen at 0.1 mg/kg in some cases. The authors also note "dehydration was observed due to the exaggerated PD response (i.e., diarrhea) at the studied dose (30 mg/kg).
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    The potency of Tenapanor was tested against NHE1, NHE2, NHE3, NaPiIIb, TGR5, ASBT, and Pit-1. Exclud ...

    Potency
    Cellular
    In Vitro

    SLC9A3

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.2c00037

    In Vivo Validations

    Rat
    Dose: 1-30 mg/Kg
    Route of delivery: Oral
    Cmax: <3 ng/mL

    DOI Reference: 10.1021/acsmedchemlett.2c00037

    Mouse
    Dose: 1-10 mg/Kg
    Route of delivery: Oral
    Cmax: <1 ng/mL

    DOI Reference: 10.1126/scitranslmed.3007790

    Chemical Information

    Molecular Formula C50H66Cl4N8O10S2
    SMILEs CN1Cc2c(Cl)cc(Cl)cc2[C@H](c2cccc(S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)c3cccc([C@@H]4CN(C)Cc5c(Cl)cc(Cl)cc54)c3)c2)C1
    InChI InChI=1S/C50H66Cl4N8O10S2/c1-61-31-43(41-27-37(51)29-47(53)45(41)33-61)35-7-5-9-39(25-35)73(65,66)59-15-19-71-23-21-69-17-13-57-49(63)55-11-3-4-12-56-50(64)58-14-18-70-22-24-72-20-16-60-74(67,68)40-10-6-8-36(26-40)44-32-62(2)34-46-42(44)28-38(52)30-48(46)54/h5-10,25-30,43-44,59-60H,3-4,11-24,31-34H2,1-2H3,(H2,55,57,63)(H2,56,58,64)/t43-,44-/m0/s1
    Molecular weight 1142.31 Da
    AlogP 6.156600000000009
    HBond acceptors 18
    HBond donors 6
    Atoms 140

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    Expert Reviews

    by SERP
    (on 27 Jun 2022)
    In Model Organisms
    Tenapanor is an approved drug targeting the Intestinal Na+/H+ Exchanger Isoform 3 (SLC9A3/NHE3). It has excellent selectivity versus other intestinal transporters and is well tolerated. Rats appear to...
    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