1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Felcisetrag

Felcisetrag (Synonyms: TD-8954)

Cat. No.: HY-102057
Handling Instructions

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.

For research use only. We do not sell to patients.

Felcisetrag Chemical Structure

Felcisetrag Chemical Structure

CAS No. : 916075-84-8

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Description

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.

IC50 & Target[1]

huamn 5-HT4(c) Receptor

9.4 (pKi)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Guinea pigs[1]
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[1]
Dosage: 0.03~10 mg/kg
Administration: Intraduodenal administration
Result: Evoked a dose-dependent relaxation of the esophagus.
Animal Model: Dogs[1]
Dosage: 10 and 30 μg/kg
Administration: P.o
Result: Produced an increase in contractility of the antrum, duodenum, and jejunum.
Molecular Weight

455.59

Formula

C₂₅H₃₇N₅O₃

CAS No.
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Felcisetrag
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