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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-NURR1 (NR4A2)-4A7C-301
4A7C-301

Chemical Structure : 4A7C-301

CAS No.:

4A7C-301

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

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

参考文献

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

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