4A7C-301

Chemical Structure : 4A7C-301

CAS No.:

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货号: PC-21004Not For Human Use, Lab Use Only.

4A7C-301 is a potent, selective, brain-penetrant agonist of nuclear receptor Nurr1 with EC50 of 6.53 uM, binds to Nurr1 ligand binding domain (LBD) with IC50 of 50 nM.

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5 mg	￥1180	In stock
10 mg	￥1780	In stock
25 mg	￥2980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

4A7C-301 is a potent, selective, brain-penetrant agonist of nuclear receptor Nurr1 with EC50 of 6.53 uM, binds to Nurr1 ligand binding domain (LBD) with IC50 of 50 nM.
4A7C-301 shows higher potency than chloroquine (CQ), exhibits approximately 50 times higher potency than CQ in N27-A cells (EC50= ~0.2 and ~10 µM, respectively).
4A7C-301 selectively activates the transcriptional activity of Nurr1, but not Nur77, over Nor1.
4A7C-301 induces Nurr1's transcriptional activity with the greatest potency (13-14 fold) among NR4A members in SK-N-BE(2)C cells.
4A7C-301 restores Nurr1 protein expression levels that are diminished by exposure to environmental and genetic risk factors of PD in vitro.
4A7C-301 suppresses neuroinflammation in ventral mesencephalic (VM) neuron-glia co-cultures.
4A7C-301 restores autophagy against MPP+ in vitro.
4A7C-301 (5 mg/kg/day) 4A7C-301 protects midbrain dopamine neurons in the MPTP-induced male mouse model of PD and improves both motor and non-motor olfactory deficits without dyskinesia-like behaviors.
4A7C-301 also significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models.

物理化学性质&存储条件

分子量	524.11
分子式	C27H38ClN9
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	N1-(4,6-bis(4-ethylpiperazin-1-yl)pyrimidin-2-yl)-N2-(7-chloroquinolin-4-yl)ethane-1,2-diamine

参考文献

1. Woori Kim, et al. Nat Commun. 2023 Jul 18;14(1):4283.

4A7C-301

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物理化学性质&存储条件

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4A7C-301

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物理化学性质&存储条件

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