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NURR1-Ant-29 | NURR1-Ant-29 : Agonist of NR4A2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NR4A2
  • IC50:300 nM
  • EC50:110 nM
  • EC50:220 nM
Agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective 15x over DHODH inhibitory potency (IC50 = 1.7 ± 0.4 μM), and >10-fold selectivity over Nur ...

Potency
Cellular
In Vitro

NR4A2

Mode of Action: Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c00415

In Vivo Validations

Rat
Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 4.4 h
Cmax: 56 uM
Area Under the Curve:: 290 uM*h
Bioavailability: 89%

DOI Reference: 10.1021/acs.jmedchem.3c00415

Chemical Information

Molecular Formula C22H18FNO4
SMILEs C#CCOc1cccc(-c2ccc(NC(=O)C3=C(C(=O)O)CCC3)c(F)c2)c1
InChI InChI=1S/C22H18FNO4/c1-2-11-28-16-6-3-5-14(12-16)15-9-10-20(19(23)13-15)24-21(25)17-7-4-8-18(17)22(26)27/h1,3,5-6,9-10,12-13H,4,7-8,11H2,(H,24,25)(H,26,27)
Molecular weight 379.12 Da
AlogP 4.008300000000002
HBond acceptors 5
HBond donors 2
Atoms 46

Expert Reviews

No SERP comments found for NURR1-Ant-29

Probe NURR1-Ant-29 is in the process of SERP review.

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