| Identification | Back Directory | [Name]
TD-8954 | [CAS]
916075-84-8 | [Synonyms]
TD-8954
Felcisetrag
1-Piperidinecarboxylic acid, 4-[[4-[[[[2-(1-methylethyl)-1H-benzimidazol-7-yl]carbonyl]amino]methyl]-1-piperidinyl]methyl]-, methyl ester | [Molecular Formula]
C25H37N5O3 | [MDL Number]
MFCD28502286 | [MOL File]
916075-84-8.mol | [Molecular Weight]
455.59 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (109.75 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | 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.
|
| [IC 50]
huamn 5-HT4(c) Receptor: 9.4 (pKi) | [storage]
Store at -20°C | [References]
[1] Beattie DT, et al. The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011;2:25. DOI:10.3389/fphar.2011.00025 |
|
|