nurr 1

Nurr1 agonist 8 is a low-affinity Nurr1 agonist that can be used to study neurological diseases such as Parkinson's.

Nurr1 agonist 7 (compound 110) is an agonist targeting the Nurr1 receptor, exhibiting an EC50 of 0.12 μM [1].

Nurr1 agonist 12 (Compound 37) acts as an agonist of the nuclear receptor-related protein 1 (Nurr1), enhancing its transcriptional activity with an EC50 of 0.06 μM. It stimulates human response elements NBRE, NurRE, and DR5 with EC50 values of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Additionally, Nurr1 agonist 12 induces the expression of neurotrophic genes regulated by Nurr1, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). The compound also demonstrates neuroprotective effects against neurotoxicity caused by Paraquat.

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 Parkinson's disease organoid models and can penetrate the human brain endothelial cell barrier.

Nurr1 agonist 10 (compound 37) is a potent Nurr1 activator with an EC50 of 40 nM. It has potential applications in the research of Parkinson's disease and Alzheimer's disease.

Nurr1 agonist 13 (Compound 1) is a potent agonist of the nuclear receptor-related 1 (Nurr1, NR4A2), with an EC50 value of 0.06 μM. It holds promise for research on neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and multiple sclerosis.

Nurr1 Agonist 14 (Compound 32) is a Nurr1 agonist with an EC50 of 0.09 μM for Nurr1. It exhibits significant neuroprotective activity without being hindered by residual DHODH inhibition. This compound can upregulate neuroprotective genes in dopaminergic neurons, such as SOD2, SESN3, BIRC5, XIAP, FLRT2, and CRMP4. Nurr1 Agonist 14 is useful for studying neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and multiple sclerosis (MS).

Nurr1 agonist 1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1 which is an appealing target to treat neurodegenerative diseases.

Nurr1 inverse agonist-1 is a indole-based inverse agonist targeting the neuroprotective transcription factor Nurr1, which plays a pivotal role in dopaminergic neuron regulation. Nurr1 inverse agonist-1 decreases the receptor's intrinsic transcriptional activity by up to more than 90% and revealed preference for inhibiting Nurr1 monomer activity. Nurr1 inverse agonist-1 enables the mechanistic study of Nurr1-mediated gene repression and the exploration of its potential implications in neurodegenerative disorders such as Parkinson’s disease.

Nurr1 agonist 4 (compound 8) is a potent Nurr1 agonist with an EC50 value of 2.1 μM [1].

Compound 13, a Nurr1 agonist, exhibits a dissociation constant (Kd) of 1.5 μM and an effective concentration for 50% response (EC50) of 3 μM [1].

Compound 5o, a Nurr1 agonist, exhibits neuroprotective properties as a transcription factor Nurr1 agonist, possessing a dissociation constant (Kd) of 0.5 μM and a half-maximal effective concentration (EC50) of 3 μM [1].

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.

IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.

C-DIM12 induced expression of Nurr1-regulated genes. C-DIM12 increased expression of transfected human Nurr1, induced Nurr1 protein expression in primary dopaminergic neurons and enhanced neuronal survival from exposure to 6-OHDA.

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Nurr1 agonist 2 is a Nurr1 agonist with an EC50 value of 0.07 μM. Nurr1 agonist 2 increases the mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand-binding domain (LBD) with a Kd of 0.14 μM. Nurr1 agonist 2 can be used to study parkinsonism.

Nurr1 Agonist 11 (compound 53) is an effective selective agonist for Nurr1 with an IC50 of 26 µM. This compound also demonstrates the capacity to cross the blood-brain barrier (BBB) in cell models.