T0901317

Agonist of NR1H2, NR1H3

Structure

Information

  • NR1H2
  • NR1H3
  • Agonist
  • 5 -10 uM
  • Reviewer recommended concentration: up to 1 uM

In Vitro Validations

Uniprot ID: P55055
Target Class: NHR
Target SubClass: NR1 Subfamily
Potency: IC 50
Potency Value: 20 nM
Potency Assay: Scintillation proximity assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Available through the years in multiple papers.
Target aliases:
Oxysterols receptor LXR-beta, UNR, NER, LXRB, NR1H ...

DOI Reference: 10.1126/science.289.5484.1524

Uniprot ID: P55055
Target Class: NHR
Target SubClass: NR1 Subfamily
Potency: IC 50
Potency Value: 10 nM
Potency Assay: FRET-based co-activator (SRC-1) recruitment assay measuring agonist activity
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Oxysterols receptor LXR-beta, UNR, NER, LXRB, NR1H ...

DOI Reference: 10.1126/science.289.5484.1524

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and no activity against other receptors (FXR, RXRalpha, PPARalpha, PPARdelta, PPARgamma, CAR, ERRalpha, CPF, HNF4alpha, RORalpha, Nor1, Nurf1, COUPTFII, RORg (204 nM)
Potency assay, off target (cells): In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and no activity against other receptors (FXR, RXRalpha, PPARalpha, PPARdelta, PPARgamma, CAR, ERRalpha, CPF, HNF4alpha, RORalpha, Nor1, Nurf1, COUPTFII
Probe Selectivity in Cell:
In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and no activity against other receptors (FXR, RXRalpha, PPARalpha, PPARdelta, PPARgamma, CAR, ERRalpha, CPF, HNF4alpha, RORalpha, Nor1, Nurf1, COUPTFII
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Probe is highly specific for LXR amongst all steroid hormone receptors tested. Agonist is able to activate LXR target genes and reporters in cell lines and in mice.

(last updated: 15 Sept 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

T 0901317 is a widely used chemical probe for LXRa/LXRb. It has good potency and selectivity across the nuclear hormone receptor family if used at the appropriate concentrations (maximum 1uM in cells). At high micromolar concentrations, cross-reactivity has been noted on RORa doi: 10.1124/mol.109.060905. T 0901317 can be used as an in vivo chemical probe by oral administration in mice and rats.

(last updated: 4 Nov 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

T0901317 is a selective probe for LXRα and LXRβ. Although there is no data for selectivity outside of the target family, selectivity across the nuclear hormone receptor family is good within appropriate concentrations (see RORα/γ as exceptions). The probe may also exert acute effects nongenomic in nature and alterations in β-Cell function should be considered at higher concentrations, DOI: 10.1210/en.2016-1941.

(last updated: 4 May 2021 )