Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | 5-HT4C 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] |
別名 | TD 8954, TD8954, TD-8954 |
分子量 | 455.59 |
分子式 | C25H37N5O3 |
CAS No. | 916075-84-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.0 mg/mL (98.8 mM ), Sonication and heating to 60℃ are recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Felcisetrag 916075-84-8 GPCR/G Protein Neuroscience 5-HT Receptor TD 8954 TD8954 TD-8954 Inhibitor inhibitor inhibit