费西塞拉 T28934

Product Introduction
Bioactivity


英文名: Felcisetrag

描述: Felcisetrag (TD-8954) 是一种有效且选择性的口服活性 5-HT4 受体激动剂，具有胃肠道促动力特性。Felcisetrag 对人类重组 5-HT4(c) (h5-HT4(c)) 受体显示出高亲和力 ，pKi 为9.4。

体外活性: Felcisetrag在表达h5-HT4(c)受体的HEK-293细胞中诱导cAMP水平增加（pEC50 =9.3），并在豚鼠结肠纵向肌/神经丛制备中引起收缩（pEC50 =8.6）。体外实验显示，Felcisetrag表现出中等固有活性。[1]

体内活性: The administration of Felcisetrag (0.033 mg/kg; s.c.) results in an acceleration of carmine red dye colonic transit, leading to a decrease in excretion time.[1] A dose-dependent relaxation of the esophagus is induced by Felcisetrag (0.03~10 mg/kg; intraduodenal administration).[1] Felcisetrag (10 and 30 μg/kg; p.o) elicits an increase in contractility in the antrum, duodenum, and jejunum.[1]

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

溶解度: DMSO : 45.0 mg/mL (98.8 mM )


关键字: Felcisetrag

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相关库: Drug Repurposing Compound Library | Neurotransmitter Receptor Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Bioactive Compound Library

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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