产品
编 号：F519175
分子式：C25H37N5O3
分子量：455.59
分子式：C25H37N5O3
分子量：455.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 916075-84-8
产品详情
生物活性：
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
体内研究：
Felcisetrag (0.03~3?mg/kg; s.c.) increases the colonic transit of carmine red dye, reducing the time taken for its excretion.Felcisetrag (0.03~10?mg/kg; intraduodenal administration) evokes a dose-dependent relaxation of the esophagus.Felcisetrag (10 and 30?μg/kg; p.o) produces an increase in contractility of the antrum, duodenum, and jejunum.Animal Model:Guinea pigs
Dosage:0.03~3?mg/kg
Administration:S.c.
Result:Increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
Animal Model:Rats
Dosage:0.03~10?mg/kg
Administration:Intraduodenal administration
Result:Evoked a dose-dependent relaxation of the esophagus.
Animal Model:Dogs
Dosage:10 and 30?μg/kg
Administration:P.o
Result:Produced an increase in contractility of the antrum, duodenum, and jejunum.
体外研究：
Felcisetrag produces an elevation of cAMP in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50?=?9.3), and contracts the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50?=?8.6). Felcisetrag has moderate intrinsic activity in the vitro assays.
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
体内研究：
Felcisetrag (0.03~3?mg/kg; s.c.) increases the colonic transit of carmine red dye, reducing the time taken for its excretion.Felcisetrag (0.03~10?mg/kg; intraduodenal administration) evokes a dose-dependent relaxation of the esophagus.Felcisetrag (10 and 30?μg/kg; p.o) produces an increase in contractility of the antrum, duodenum, and jejunum.Animal Model:Guinea pigs
Dosage:0.03~3?mg/kg
Administration:S.c.
Result:Increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
Animal Model:Rats
Dosage:0.03~10?mg/kg
Administration:Intraduodenal administration
Result:Evoked a dose-dependent relaxation of the esophagus.
Animal Model:Dogs
Dosage:10 and 30?μg/kg
Administration:P.o
Result:Produced an increase in contractility of the antrum, duodenum, and jejunum.
体外研究：
Felcisetrag produces an elevation of cAMP in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50?=?9.3), and contracts the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50?=?8.6). Felcisetrag has moderate intrinsic activity in the vitro assays.
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