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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

      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 public 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