BRF110 | Nurr1-RXRα agonist | Probechem Biochemicals

Chemical Structure : BRF110

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BRF110 (BRF-110, BRF 110)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	413.40
分子式	C22H18F3N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-((5-allyl-2-phenyl-6-(trifluoromethyl)pyrimidin-4-yl)(methyl)amino)benzoic acid

参考文献

1. Spathis AD, et al. Proc Natl Acad Sci U S A. 2017 Apr 11;114(15):3999-4004.

BRF110 (BRF-110, BRF 110)

生物&药学活性

物理化学性质&存储条件

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BRF110 (BRF-110, BRF 110)

生物&药学活性

物理化学性质&存储条件

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