Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T77549 |
Nurr1 agonist 2
|
Others | Others |
Nurr1 agonist 2 是一种 Nurr1 激动剂 ,EC50 值为 0.07 μM。Nurr1 agonist 2 增加 Nurr1 调节基因酪氨酸羟化酶 (TH) 和囊泡氨基酸转运蛋白 2 (VMAT2) 的 mRNA 表达。Nurr1 agonist 2 与重组 Nurr1 配体结合域 (LBD) 结合,Kd 值为 0.14 μM。Nurr1 agonist 2 可用于研究帕金森综合征。 | |||
T81635 | Nurr1 agonist 5 | ||
Nurr1 agonist 5 (compound 5o)为具神经保护性的Nurr1转录因子激动剂,其Kd值为0.5 μM,EC50值为3 μM。 | |||
T81632 |
Nurr1 agonist 8
|
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Nurr1 agonist 8 (compound 111) 以0.09 μM的EC50表现出Nurr1激动活性。 | |||
T81634 | Nurr1 agonist 6 | ||
Nurr1 agonist 6 (compound 13)作为Nurr1激动剂,展现了Kd 1.5 μM和EC50 3 μM的亲和力与效应浓度。 | |||
T81633 |
Nurr1 agonist 7
|
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Nurr1 agonist 7 (compound 110)作为一种Nurr1的激动剂,其EC50值为0.12 μM。 | |||
T60443 | Nurr1 agonist 1 | ||
Nurr1 agonist 1 是一种神经保护的转录因子Nurr1的反向激动剂工具,Nurr1 是治疗神经退行性疾病的有吸引力的靶点。 | |||
T78088 |
Nurr1 agonist 4
|
Others | Others |
Nurr1激动剂4(化合物8)是一种具有高亲和力的化合物,其EC50值为2.1μM。 | |||
T78049 |
Nurr1 inverse agonist-1
|
Others | Others |
Nurr1 inverse agonist-1为Nurr1, 一种具有神经保护功能的转录因子, 的反向激动剂。 | |||
T8381 |
Amodiaquine
|
Others; Histone Methyltransferase; Parasite | Chromatin/Epigenetic; Microbiology/Virology; Others |
Amodiaquine 是一种合成的4-氨基喹啉类抗疟剂,是一种有口服活性的组胺 N-甲基转移酶抑制剂。它也是一种Nurr1激动剂,有抗炎活性,可特异性结合Nurr1的配体结合域,EC50约为20 μM。 | |||
T83894 |
4A7C-301-Nurr1 Agonist
4A7C-301-Nuclear Receptor-Related 1 |
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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。 | |||
T27620 |
IP7e
IP 7e,IP-7e,isoxazolo-pyridinone 7e |
Others | Others |
IP7e (isoxazolo-pyridinone 7e) 是一种 Nurr1 激活剂,EC50 值为 3.9 nM。 | |||
T0381 |
Amodiaquine dihydrochloride dihydrate
Amodiaquine hydrochloride,阿莫地喹盐酸盐,Amodiaquin dihydrochloride dihydrate |
Histone Methyltransferase; Parasite; Histamine Receptor | Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) 是一种具有口服活性的组胺 N-甲基转移酶抑制剂,也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM。它是 4-氨基喹啉衍生物,具有抗疟和抗炎特性。 | |||
T3106 |
C-DIM12
|
Apoptosis; Others | Apoptosis; Others |
C-DIM12是一种人工合成的Nurr1激活剂,可诱导Nurr1和DA 基因表达。 | |||
T35159 |
XCT0135908
XCT 0135908,XCT-0135908 |
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XCT0135908 is a selectivity agonist of RXR -Nurr1 over a broad range of other RXR dimerization partners but with a rather low potency. | |||
T70237 |
HX-600
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HX-600 is a synthetic agonist for the RXR-Nurr1 heterodimer complex. HX-600 prevents ischemia-induced neuronal damage. | |||
T22242 |
Amodiaquine hydrochloride
|
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Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂,是一种有效的口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂,Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM,具有抗炎作用。 | |||
T83328 | 4A7C-301 | ||
4A7C-301是一种Nurr1激动剂,体外显示出强大的神经保护能力。在AAV2介导的α-突触核蛋白过表达雄鼠模型中,该化合物能显著纠正神经病理学异常,并改善运动及嗅觉功能障碍。此外,4A7C-301适用于帕金森病相关研究。 | |||
T69921 |
BRF110
|
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BRF110 is a brain penetrant, potent and selective agonist of nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) heterodimer. BRF110 is a neuroprotective agent that prevents dopaminergic neuron demise and striatal dopaminergic denervation in vivo against PD-causing toxins. It induced dopamine biosynthesis in vivo. BRF110 chronic dosing does not induce dyskinesia in mice model. |