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4A7C-301-Nurr1激动剂是一种核受体相关1(Nurr1)的激动剂。它通过与Nurr1配体结合域(LBD;IC50 = 48.22 nM)结合,增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性(EC50s = 6.53 和 50-70 µM,分别)。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡,并减少运动和嗅觉缺陷,而不诱发类似运动障碍的行为。
4A7C-301-Nurr1激动剂是一种核受体相关1(Nurr1)的激动剂。它通过与Nurr1配体结合域(LBD;IC50 = 48.22 nM)结合,增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性(EC50s = 6.53 和 50-70 µM,分别)。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡,并减少运动和嗅觉缺陷,而不诱发类似运动障碍的行为。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 455 | 35日内发货 | |
1 mg | ¥ 682 | 35日内发货 | |
5 mg | ¥ 2,920 | 35日内发货 |
产品描述 | The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein. |
别名 | 4A7C-301-Nuclear Receptor-Related 1 |
分子量 | 524.10 |
分子式 | C27H38ClN9 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMF: 20 mg/ml Ethanol: 30 mg/ml DMSO: 20 mg/ml |
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