NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd 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 Parkinsons disease, dementia and multiple sclerosis[1].
Molekulargewicht:
421.78
Formel:
C20H14ClF2NO5
Target-Kategorie:
Nuclear Hormone Receptor 4A/NR4A
Anwendungsbeschreibung:
MCE Product type: Reference compound
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