SR9238 |
SR9238 : Inverse Agonist of NR1H2, NR1H3
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 |
| |
| NR1H3 |
|
Inverse Agonist
up to 10 uM
Selectivity
In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectively inhibits liver LXR over peripheral LXR.
Outside target family:
No activity in a panel of ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Nuclear receptor specificity panel illustrating the specificity of SR9238. A Gal4-NR LBD cell-based ...
Potency Cellular
In Vitro
NR1H2
Mode of Action: Inverse Agonist
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/cb300541g
NR1H3
Mode of Action: Inverse Agonist
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/cb300541g
In Vivo Validations
Mouse
Dose: 30 mg/Kg/Day
Route of delivery:
Intraperitoneal
Organ of interest (O):
Liver
Target engagement assay:
SR9238 suppresses the expression of lipogenic enzyme and proinflammatory cytokine genes in an animal model of hepatic steatosis.
DOI Reference: 10.1021/cb300541g
Negative Control Compounds
Chemical Information
| Molecular Formula | C31H33NO7S2 |
| SMILEs | CCOC(=O)c1ccc(CN(Cc2ccc(-c3cccc(S(C)(=O)=O)c3)cc2)S(=O)(=O)c2c(C)cc(C)cc2C)o1 |
| InChI | InChI=1S/C31H33NO7S2/c1-6-38-31(33)29-15-14-27(39-29)20-32(41(36,37)30-22(3)16-21(2)17-23(30)4)19-24-10-12-25(13-11-24)26-8-7-9-28(18-26)40(5,34)35/h7-18H,6,19-20H2,1-5H3 |
| Molecular weight | 595.17 Da |
| AlogP | 5.84316 |
| HBond acceptors | 8 |
| HBond donors | -- |
| Atoms | 74 |
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