化合物DA-6886 T27117

Product Introduction
Bioactivity


英文名: DA-6886

描述: DA-6886 是一种 5-羟色胺受体 4（5-HT4）激动剂。DA-6886 以 5-HT4 受体拮抗剂敏感的方式诱导大鼠食道制剂松弛。在表达 hERG 通道的 CHO 细胞中对 DA-6886 进行的评估显示，它抑制 hERG 通道电流的 pIC50 值为 4.3，表明该化合物对 5-HT4 受体的选择性比 hERG 通道高 1000 倍。

体内活性: In the normal ICR mice, DA-6886 (0.4 and 2mg/kg; oral) resulted in a marked stimulation of colonic transit. In the loperamide-induced constipation mouse model, DA-6886 (2mg/kg) significantly improved the delay of colonic transit. Taken together, DA-6886 is a highly potent and selective 5-HT4 receptor agonist to accelerate colonic transit in mice, which might be a therapeutic agent having a favorable safety profile in the treatment of gastrointestinal motor disorders such as IBS-C and chronic constipation.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (101.5 mM)


关键字: DA-6886

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途