1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Nuclear Hormone Receptor 4A/NR4A RAR/RXR
  3. Nurr1/RXR agonist 1

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with Ks of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research.

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Nurr1/RXR agonist 1

Nurr1/RXR agonist 1 Chemical Structure

CAS No. : 2231746-53-3

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Description

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with K[1]s of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research[1].

IC50 & Target[1]

Nurr1/NR4A2

 

In Vitro

Nurr1/RXR agonist 1 (compound 2) (15 h) induces a considerable 3.3-fold activation of Nurr1, with both Nurr1 and RXR involved[1].
Nurr1/RXR dual agonist 1 (30 μM) diminishes Nurr1 homodimer formation while leaving the Nurr1:RXR heterodimer intact[1].
Nurr1/RXR agonist 1 (0.3-30 μM) enhances DR5-dependent transcription but does not activate NBRE or NurRE[1].
Nurr1/RXR agonist 1 (0.3-30 μM, 24 h) exhibits no toxic effect in HEK293T cells[1].
Nurr1/RXR agonist 1 (10 μM, 21 h) achieves differential modulation or functional selectivity in activating downstream gene expression programs in rat dopaminergic neurons[1].
Nurr1/RXR agonist 1 induces genes that have a higher empirical probability of containing DR5 elements in their promoter regions[1].

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

Real Time qPCR[1]

Cell Line: rat dopaminergic neurons
Concentration: 10 μM
Incubation Time: 21 h
Result: Induced the expression of tyrosine hydroxylase (TH), fibronectin leucine rich transmembrane protein 2 (FLRT2), brain-derived neurotrophic factor (BDNF) and collapsin response mediator protein 4 (CRMP4; Dpysl3 in rat).
Did not induced X-linked inhibitor of apoptosis protein (XIAP), sestrin 3 (SESN3), cyclin D2 (CCND2), baculoviral inhibitor of apoptosis repeat-containing 5 (BIRC5), and superoxide dismutase 2 (SOD2).
Molecular Weight

319.35

Formula

C18H19F2NO2

CAS No.
SMILES

O=C(O)CC1=CC=C(N2C(C)=C(C)C3=C2CCC(F)(F)C3)C=C1

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nurr1/RXR agonist 1
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HY-180576
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