Velusetrag | 5-HT4 agonist | Probechem Biochemicals

Chemical Structure : Velusetrag

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Velusetrag (TD-5108, TD5108)

货号: 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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生物&药学活性

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.
Velusetrag (TD-5108) displays >25-fold selectivity over other biogenic amine receptors, and no effect on hERG channels.
Velusetrag (TD-5108) 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.

物理化学性质&存储条件

分子量	504.646
分子式	C25H36N4O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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.

Velusetrag (TD-5108, TD5108)

生物&药学活性

物理化学性质&存储条件

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Velusetrag (TD-5108, TD5108)

生物&药学活性

物理化学性质&存储条件

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