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Velusetrag hydrochloride

Names

[ CAS No. ]:
866933-51-9

[ Name ]:
Velusetrag hydrochloride

[Synonym ]:
NF4JCT94PW
3-Quinolinecarboxamide, 1,2-dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-methylethyl)-2-oxo-, hydrochloride (1:1)
Velusetrag hydrochloride
N-[(3-endo)-8-{(2R)-2-Hydroxy-3-[methyl(methylsulfonyl)amino]propyl}-8-azabicyclo[3.2.1]oct-3-yl]-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide hydrochloride (1:1)

Biological Activity

[Description]:

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

[References]

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. View Related Products by Target 5-HT Receptor Other Indication

Chemical & Physical Properties

[ Molecular Formula ]:
C25H37ClN4O5S

[ Molecular Weight ]:
541.103

[ Exact Mass ]:
540.217346

Related Compounds