Felcisetrag

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Felcisetrag (TD-8954) 是一种具有口服活性，有效和选择性 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)) 受体具有高亲和力 (pKi =9.4)。

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.

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 (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 pigsDosage: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.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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916075-84-8

455.59

C25H37N5O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (109.75 mM; 超声助溶 (<60°C)

COC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4nc([nH]c34)C(C)C)CC2)CC1

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(-20℃)

With Ice Pack

≥ 2 years