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Velusetrag

Chemical Structure : Velusetrag

CAS No.: 866933-46-2

Velusetrag (TD-5108)

Catalog No.: PC-62094Not For Human Use, Lab Use Only.

Velusetrag (TD-5108) is a potent, selective and oral 5-HT4 receptor agonist with pKi of 7.7, shows >500-fold selectivity over other 5-HT receptors.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Velusetrag (TD-5108) is a potent, selective and oral 5-HT4 receptor agonist with pKi of 7.7, shows >500-fold selectivity over other 5-HT receptors; displays >25-fold selectivity over other biogenic amine receptors, and no effect on hERG channels; increases the contractility of the canine antrum, duodenum and jejunum with higher potency than tegaserod, demonstrates robust in vivo activity in the guinea pig, rat and dog gastrointestinal tracts.

Other Indication

Phase 2 Clinical

Physicochemical Properties

M.Wt 504.646
Formula C25H36N4O5S
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

N-((1R,3R,5S)-8-((R)-2-hydroxy-3-(N-methylmethylsulfonamido)propyl)-8-azabicyclo[3.2.1]octan-3-yl)-1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxamide

References

1. Beattie DT, et al. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47.

2. Smith JA, et al. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.

3. Manini ML, et al. Neurogastroenterol Motil. 2010 Jan;22(1):42-9, e7-8.

4. Long DD, et al. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6048-52.

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