Biological Activity
MRL871 (MRL-871) is an allosteric RORγt ligand used in nuclear-receptor research. Independent work also identified PPARγ partial agonism. MRL-871 IC50 was 7 ± 1 nM; the structurally related MRL-058 and MRL-003 had weaker activity.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Cofactor recruitment | RORγt AlphaScreen coactivator-peptide assay. [1], Fig. 2 | MRL-871 IC50 was 7 ± 1 nM; the structurally related MRL-058 and MRL-003 had weaker activity. |
| Allosteric antagonism | RORγt ligand-binding domain with increasing cholesterol. [1] | MRL-871 inhibition was largely independent of cholesterol concentration, consistent with a separate allosteric pocket and altered helix-12 conformation. |
| Cellular response | RORγt-regulated IL17A transcription assays. [1] | Reduced IL17A mRNA supported cellular functional activity. |
| Additional pharmacology | Independent PPARγ study. [2] | MRL-871 also exhibited partial agonism at PPARγ; it is not an exclusively RORγt-selective probe. |
In Vivo
No compound-specific animal efficacy result is established by the sources summarized here.
Interpretation
MRL871 should not be treated as an exclusively selective RORγt probe.
