Felcisetrag
CAS No. : 916075-84-8
(Synonyms: TD-8954)
| Size | Price | Stock |
|---|---|---|
| 5mg | $480 | In-stock |
| 10mg | $800 | In-stock |
| 25mg | $1650 | In-stock |
| 50mg | $2600 | In-stock |
| 100mg | $4000 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-102057 |
| M.Wt: | 455.59 |
| Formula: | C25H37N5O3 |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (109.75 mM; ultrasonic and warming and heat to 60°C) |
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: pKi: 9.4(h5-HT4(c))[1].
pEC50: 9.3 (h5-HT4(c) in HEK-293 cells)[1]
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].
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].
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