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Felcisetrag

Catalog No. T28934 CAS 916075-84-8

Synonyms: TD 8954, TD8954, TD-8954

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.

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Felcisetrag, CAS 916075-84-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 157.00
5 mg	In stock	$ 397.00
10 mg	In stock	$ 589.00
25 mg	In stock	$ 945.00
50 mg	In stock	$ 1,280.00
100 mg	In stock	$ 1,730.00
500 mg	In stock	$ 3,460.00
1 mL * 10 mM (in DMSO)	In stock	$ 437.00

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Purity: 100%

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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-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]

Synonyms	TD 8954, TD8954, TD-8954
Molecular Weight	455.59
Formula	C25H37N5O3
CAS No.	916075-84-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (98.8 mM ), Sonication and heating to 60℃ are recommended.

References and Literature

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. 2. Mozaffari S, et al. Phase II drugs under clinical investigation for the treatment of chronic constipation. Expert Opin Investig Drugs. 2014;23(11):1485-1497. 3. Shen F, et al. 5-HT(4) receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: A pharmacodynamic and pharmacokinetic assessment. Neuropharmacology. 2011;61(1-2):69-79. 4. McKinnell RM, et al. Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. Bioorg Med Chem Lett. 2013;23(14):4210-4215.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Clinical Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library

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Keywords

Felcisetrag 916075-84-8 GPCR/G Protein Neuroscience 5-HT Receptor TD 8954 TD8954 TD-8954 inhibitor inhibit

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