nurr1

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

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 Inverse Agonist-1 is an inverse agonist for the neuroprotective transcription factor Nurr1, serving as a research tool.

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].

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

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

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

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.

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].

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

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.

Prostaglandin E2-biotin, an analog of prostaglandin, is utilized in the research of Nurr1-related diseases, including cancer and autoimmune diseases [1].

BRF110 is a brain penetrant, potent and selective agonist of nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) heterodimer. BRF110 is a neuroprotective agent that prevents dopaminergic neuron demise and striatal dopaminergic denervation in vivo against PD-causing toxins. It induced dopamine biosynthesis in vivo. BRF110 chronic dosing does not induce dyskinesia in mice model.

Anticanceragent 257 (compound of formula (I)) is an anticancer agent that regulates Nur77 and Nurr1.

BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R cAMP PKA Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.

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

17-trans Prostaglandin E3, a prostaglandin analog, stimulates Nurr1-dependent transcriptional activity and can be utilized for researching conditions associated with Nurr1, including cancer and autoimmune diseases [1].

XCT0135908 is a selectivity agonist of RXR -Nurr1 over a broad range of other RXR dimerization partners but with a rather low potency.

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

HX-600 is a synthetic agonist for the RXR-Nurr1 heterodimer complex. HX-600 prevents ischemia-induced neuronal damage.

4A7C-301, a Nurr1 agonist, exhibits potent neuroprotective effects in vitro and markedly mitigates neuropathological abnormalities while enhancing motor and olfactory functions in male mouse models with AAV2-mediated α-synuclein overexpression. This compound is applicable in Parkinson's disease research [1].

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, is an antimalarial agent that also acts as a potent oral histamine N-methyltransferase inhibitor with a K i value of 18.6 nM. Additionally, it functions as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, demonstrating anti-inflammatory effects [1] [2] [3] [4] [5].

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.