Velusetrag

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Velusetrag (TD-5108) 是一种有效的、选择性的口服 5-HT4 受体激动剂，pKi 为 7.7。

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.

Velusetrag (10 pM-100 μM) concentration-dependently increases the cAMP in HEK-293 cells stably transfected with the h5-HT4(c) receptor, with a pEC50 of 8.3.Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC50 of 7.9.Velusetrag (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC50 of 7.9.

Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice.Velusetrag (3 mg/kg; a single i.p.) increases hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.Velusetrag (0.003-3 mg/kg; a single s.c.) increases colonic transit in a dose-dependent manner and reduces the time taken for excretion of the dye in guinea pigs.Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats. Animal Model:Male C57BL/6 mice (7-8 weeks old) were injected with MPTP Dosage:3 mg/kg Administration:A single i.p.Result:Improved facilitation of contextual fear extinction.

TD-5108

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Other Indications

Other Disease

866933-46-2

504.646

C25H36N4O5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (198.16 mM)

O=C(C1=CC2=C(N(C(C)C)C1=O)C=CC=C2)NC3CC(N4C[C@@H](O)CN(C)S(=O)(C)=O)([H])CCC4([H])C3

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

(-20℃)

With Ice Pack

≥ 2 years