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SR9243 | Inverse Agonist of NR1H2, NR1H3
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
NR1H2
    • IC 50:15 to 104 nM
    NR1H3
      • IC 50:15 to 104 nM
      Inverse Agonist
      up to 1 uM

      Selectivity

      In Cell Selectivity Assessment
      Selectivity Assessment Description:
      Specificity of SR9243 was illustrated in a cell-based co-transfection assay with 46 nuclear receptor ...

      Potency
      Cellular
      In Vitro

      NR1H2

      Mode of Action: Inverse Agonist

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.ccell.2015.05.007

      NR1H3

      Mode of Action: Inverse Agonist

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.ccell.2015.05.007

      In Vivo Validations

      Mouse
      Dose: 30, 60 mg/Kg/day
      Route of delivery: Intraperitoneal
      Organ of interest (O): Liver

      DOI Reference: 10.1016/j.ccell.2015.05.007

      Orthogonal Probes def

      T091317
      GW3965
      LXR-623

      Chemical Information

      Molecular Formula C31H32BrNO4S2
      SMILEs Cc1cc(C)c(S(=O)(=O)N(CCc2cccc(Br)c2)Cc2ccc(-c3cccc(S(C)(=O)=O)c3)cc2)c(C)c1
      InChI InChI=1S/C31H32BrNO4S2/c1-22-17-23(2)31(24(3)18-22)39(36,37)33(16-15-25-7-5-9-29(32)19-25)21-26-11-13-27(14-12-26)28-8-6-10-30(20-28)38(4,34)35/h5-14,17-20H,15-16,21H2,1-4H3
      Molecular weight 625.10 Da
      AlogP 6.878460000000008
      HBond acceptors 5
      HBond donors --
      Atoms 71

      References

      Publications

      Cross References

      canSARChEMBLPubMed

      Vendors

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      Expert Reviews

      by SERP
      (on 7 Jan 2022 )
      Cellular Use Rating
      In Model Organisms
      ( The reviewer did not leave any comments )
      by SERP
      (on 13 Jan 2022 )
      Cellular Use Rating
      In Model Organisms
      This LXR inverse agonist offers activity across a range of cell-based LXR assays, typically with EC50 values in the mid-nanomolar range. Additionally, cancer cell killing was observed, in some cases with...
      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