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T0901317 | Agonist of NR1H2, NR1H3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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 50:20 nM
  • IC 50:10 nM
  • EC 50:85 nM
NR1H3
  • IC 50:8 nM
  • EC 50:75 nM
Agonist
up to 1 uM
5 -10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and n ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and n ...
Selectivity Assessment Description:
In a panel of hormone receptors, 10 uM T0901317 showed activity against LXR-alpha>LXR-beta>PXR and n ...

Potency
Cellular
In Vitro

NR1H2

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1126/science.289.5484.1524

NR1H3

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1126/science.289.5484.1524

In Vivo Validations

Mouse
Dose: 10 mg/Kg PO, 20 mg/Kg IP, 50 mg/Kg IP
Route of delivery: Intraperitoneal, Oral
Plasma half life: 4.9 (S), 3.3 (L), 4.5 (B) h
Organ of interest (O): Serum , Liver, Brain
Target engagement assay: T0901317 increased plasma triglycerides and HDL cholesterol.

DOI Reference: 10.1126/science.289.5484.1524

Orthogonal Probes def

GW3965

Chemical Information

Molecular Formula C17H12F9NO3S
SMILEs O=S(=O)(c1ccccc1)N(CC(F)(F)F)c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1
InChI InChI=1S/C17H12F9NO3S/c18-14(19,20)10-27(31(29,30)13-4-2-1-3-5-13)12-8-6-11(7-9-12)15(28,16(21,22)23)17(24,25)26/h1-9,28H,10H2
Molecular weight 481.04 Da
AlogP 4.756400000000003
HBond acceptors 4
HBond donors 1
Atoms 43

Vendors

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Expert Reviews

by SERP
(on 15 Sept 2020 )
Cellular Use Rating
In Model Organisms
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.
by SERP
(on 4 Nov 2020 )
Cellular Use Rating
In Model Organisms
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)....
by SERP
(on 4 May 2021 )
Cellular Use Rating
In Model Organisms
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...
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