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Chemical Structure : BRF110
Catalog No.: PC-20773Not For Human Use, Lab Use Only.
BRF110 is a potent, selective, brain penetrant and vivo active agonist of Nurr1-RXRα heterodimers with EC50 of 900 nM.
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BRF110 is a potent, selective, brain penetrant and vivo active agonist of Nurr1-RXRα heterodimers with EC50 of 900 nM.
BRF110 activatesNurr1:RXRα heterodimers, but does not activate Nurr1:RXRγ heterodimers, indicating that BRF110 is specific for RXRα and does not bind to Nurr1.
BRF110 prevents DAergic neuron demise and striatal DAergic denervation in vivo against PD-causing toxins in a Nurr1-dependent manner.
BRF110 also protects against PD-related genetic mutations in patient induced pluripotent stem cell (iPSC)-derived DAergic neurons and a genetic mouse PD model.
RF110 upregulates tyrosine hydroxylase (TH), aromatic l-amino acid decarboxylase (AADC), and GTP cyclohydrolase I (GCH1) transcription, increases striatal DA in vivo.
BRF110 has symptomatic efficacy in postneurodegeneration PD models, without inducing dyskinesias on chronic daily treatment.
| M.Wt | 413.40 | |
| Formula | C22H18F3N3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Spathis AD, et al. Proc Natl Acad Sci U S A. 2017 Apr 11;114(15):3999-4004.
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