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Felcisetrag

Chemical Structure : Felcisetrag

CAS No.: 916075-84-8

Felcisetrag (TAK-954, TD-8954)

Catalog No.: PC-73307Not For Human Use, Lab Use Only.

Felcisetrag (TAK-954, TD-8954) is a highly selective and potent 5-HT4 receptor agonist with pKi of 9.4 (human 5-HT4).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Felcisetrag (TAK-954, TD-8954) is a highly selective and potent 5-HT4 receptor agonist with pKi of 9.4 (human 5-HT4).
Felcisetrag (TAK-954, TD-8954) displays high selectivity (>2,000-fold) over all other 5-HT receptors and non-5-HT receptors, ion channels, enzymes and transporters.
Felcisetrag (TAK-954, TD-8954) produced an elevation of cAMP in HEK-293 cells expressing the h5-HT(4(c)) receptor (pEC=9.3), and contracted the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50=8.6).
Felcisetrag (TAK-954, TD-8954) (0.03-3 mg/kg) increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
Felcisetrag (TAK-954, TD-8954) demonstrated robust in vivo stimulatory activity in the gastrointestinal (GI) tract of guinea pigs, rats, dogs, and humans.

Physicochemical Properties

M.Wt 455.603
Formula C25H37N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylate

References

1. Shen F, et al. Neuropharmacology. 2011 Jul-Aug;61(1-2):69-79.

2. Beattie DT, et al. Front Pharmacol. 2011 May 30;2:25.

3. Beattie DT, et al. Vascul Pharmacol. 2013 Jan;58(1-2):150-6.

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