Chemical Probes logo
LXR-623 | Partial Agonist of NR1H2, NR1H3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

More...

Targets Biochemical/Biophysical Potency Cellular Potency
NR1H2
  • IC 50:179 nM
  • EC50:6660 nM
NR1H3
  • IC 50:24 nM
  • EC50:3670 nM
Partial Agonist
up to 2 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
PPAR and FXR Gal4 transactivation assays show no agonist effects for PPARα, PPARγ, PPARδ and FXR. Bi ...

Potency
Cellular
In Vitro

NR1H2

Mode of Action: Partial Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm800799q

NR1H3

Mode of Action: Partial Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm800799q

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 7.9 h
Systemic clearance: 57 mL/min/kg
Volume of Distribution at Steady-State: 30.3 L/Kg

DOI Reference: 10.1021/jm800799q

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 5.8 h
Cmax: 633 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 3101 h·ng/mL

DOI Reference: 10.1021/jm800799q

Orthogonal Probes def

GSK2033
SR9238
T091317

Chemical Information

Molecular Formula C21H12ClF5N2
SMILEs Fc1ccc(-c2c3cccc(C(F)(F)F)c3nn2Cc2ccc(F)cc2Cl)cc1
InChI InChI=1S/C21H12ClF5N2/c22-18-10-15(24)9-6-13(18)11-29-20(12-4-7-14(23)8-5-12)16-2-1-3-17(19(16)28-29)21(25,26)27/h1-10H,11H2
Molecular weight 422.06 Da
AlogP 6.702000000000003
HBond acceptors 2
HBond donors --
Atoms 41

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

Expert Reviews

by SERP
(on 10 Nov 2020)
Cellular Use Rating
This compound is a partial agonist of LXRa making interpretation of its biology in cells very complex. Partial agonists of nuclear receptors do not make good chemical probes. I do not recommend use...
by SERP
(on 16 Nov 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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