| Name | Felcisetrag |
| Description | Felcisetrag (TD-8954) is a potent and selective orally active 5-HT4 agonist with gastrointestinal prokinetic properties.Felcisetrag shows high affinity for the human recombinant 5-HT4(c) (h5-HT4(c)) receptor with a pKi of 9.4. |
| In vitro | Felcisetrag induces an increase in cAMP levels in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50 = 9.3) and elicits contractions in the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50 = 8.6). In vitro, assays demonstrate that Felcisetrag exhibits moderate intrinsic activity.[1] |
| In vivo | The administration of Felcisetrag (0.033 mg/kg; s.c.) results in an acceleration of carmine red dye colonic transit, leading to a decrease in excretion time.[1]
A dose-dependent relaxation of the esophagus is induced by Felcisetrag (0.03~10 mg/kg; intraduodenal administration).[1]
Felcisetrag (10 and 30 μg/kg; p.o) elicits an increase in contractility in the antrum, duodenum, and jejunum.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.39 mM), Sonication is recommended.
DMSO : 45 mg/mL (98.77 mM), Sonication and heating to 60℃ are recommended.
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| Keywords | Felcisetrag | 5HTReceptor | 5-HT4 | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | pCPA methyl ester hydrochloride | 1,8-Cineole | Venlafaxine hydrochloride | Tryptamine hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | Angiogenesis related Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
