Velusetrag hydrochloride

Modify Date: 2024-01-08 22:43:05

Velusetrag hydrochloride Structure
Velusetrag hydrochloride structure
Common Name Velusetrag hydrochloride
CAS Number 866933-51-9 Molecular Weight 541.103
Density N/A Boiling Point N/A
Molecular Formula C25H37ClN4O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Velusetrag hydrochloride


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

 Names

Name Velusetrag hydrochloride
Synonym More Synonyms

 Velusetrag hydrochloride 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

 Synonyms

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)
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