NR4A agonist-2 

NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a K_d of 0.10 μM against NR4A1, and EC₅₀ values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis^[1].

NR4A agonist-2 (compound 53) (0.3-1 μM; 20 h) dose-dependently induces the mRNA expression of neuroprotective genes including BDNF, FLRT2 and SOD2 in qPCR assays using N27 rat dopaminergic neurons^[1].

NR4A agonist-2 (10 μM; 2 h) significantly inhibits the formation of Nurr1 ligand-binding domain homodimers in HTRF assays, with an inhibition rate of approximately 9-fold^[1].
In various toxicity assays of HEK293T cells treated with NR4A agonist-2 (0.1-10 μM; 24 h), the compound exerts no significant effects on cell confluency and metabolic activity, nor does it induce cell necrosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

421.78

C₂₀H₁₄ClF₂NO₅

O=C(NC1=C(C=C(C=C1)C2=C3C(OC(F)(O3)F)=CC=C2)Cl)C4=C(CCC4)C(O)=O

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• [1]. Vietor J, et al. Structural Tuning of Vidofludimus for High-Efficacy NR4A Agonism[J]. Journal of Medicinal Chemistry, 2026.