Nurr1 agonist 9 (Compound 36) acts as an agonist for Nurr1, with an EC50 of 0.090 µM and a Kd of 0.17 µM. It activates Nurr1 homodimers (NurRE, EC50 = 0.094 µM) and Nurr1-RXR heterodimers (DR5, EC50 = 0.165 µM). This compound induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in Parkinsons disease organoid models and can penetrate the human brain endothelial cell barrier.
Formel:
C21H19ClN4O2
Target-Kategorie:
NR4A
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