Felcisetrag

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)。

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库存: 现货

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5mg

￥5175.00

4140.00

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10mg

￥8637.00

6910.00

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货号: ajcx36154
CAS: 916075-84-8
别名: TD-8954
分子式: C25H37N5O3
分子量: 455.59
纯度: >98%
溶解度: DMSO : 50 mg/mL (109.75 mM; ultrasonic and warming and heat to 60°C)
储存: Store at -20°C
库存: 现货

Background

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[1].

Felcisetrag (0.03~3 mg/kg; s.c.) increases the colonic transit of carmine red dye, reducing the time taken for its excretion[1].Felcisetrag (0.03~10 mg/kg; intraduodenal administration) evokes a dose-dependent relaxation of the esophagus[1].Felcisetrag (10 and 30 μg/kg; p.o) produces an increase in contractility of the antrum, duodenum, and jejunum[1].

[1]. Beattie DT, et al. The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011;2:25.