Name: ARN25657
Brand: TargetMol
SKU: T211728
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述	ARN25657 is a dual regulator of D3R/GSK-3β. It demonstrates partial agonist activity at the D3 receptor (EC50 = 15.2 nM, Ki = 1.5 nM) alongside potent inhibitor activity against GSK-3β (IC50 = 19.3 nM). ARN25657 shows excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. It inhibits P-gp-mediated efflux of acetoxymethyl calcein, enhancing in vitro ADME properties while maintaining balanced dual-target distribution. ARN25657 is applicable in the study of bipolar disorder and related neuropsychiatric conditions.
靶点活性	D3 Receptor:15.2 nM (EC50)
体外活性	ARN25657 (Compound 16) 在 MDR1-MDCKII 细胞中以1 μM和10 μM的浓度抑制P-gp介导的乙酰氧甲基钙黄绿素外排，logD值为1.84，在10 μM时抑制率为10.9%。在神经元SH-SY5Y细胞中，ARN25657（1 μM, 5 μM, 3小时）抑制GSK-3β活性。在CHO细胞中，ARN25657（10 nM, 100 nM）对D3R表现出高亲和力，(+)-butaclamol结合抑制率为68%，K i为1.5 nM；在HEK293细胞中，对D2R表现出高亲和力，[3H]7-OH-DPAT结合抑制率为80%，K i为1 nM。ARN25657（0.1 μM, 10 μM）对FYN、PKA和CDK5/p35表现出优异的GSK-3β选择性，相较于0.1 μM的GSK-3β，其在KinaseProfiler测定中的选择性比分别为0 h、0.1 h和0 h。