Chemical Structure : BRF110
CAS No.:
2095489-35-1
BRF110
(BRF-110, BRF 110)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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413.40
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Formula
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C22H18F3N3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(O)C1=CC=C(N(C2=NC(C3=CC=CC=C3)=NC(C(F)(F)F)=C2CC=C)C)C=C1
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References
1. Spathis AD, et al. Proc Natl Acad Sci U S A. 2017 Apr 11;114(15):3999-4004.
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