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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $157 | In Stock | |
5 mg | $397 | In Stock | |
10 mg | $589 | In Stock | |
25 mg | $945 | In Stock | |
50 mg | $1,280 | In Stock | |
100 mg | $1,730 | In Stock | |
500 mg | $3,460 | In Stock | |
1 mL x 10 mM (in DMSO) | $437 | In Stock |
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. |
Targets&IC50 | 5-HT4CÂ receptor (human):9.4 (pKi) |
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] |
Alias | TD-8954, TD8954, TD 8954 |
Molecular Weight | 455.59 |
Formula | C25H37N5O3 |
Cas No. | 916075-84-8 |
Smiles | COC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4nc([nH]c34)C(C)C)CC2)CC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45.0 mg/mL (98.8 mM ), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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