Velusetrag

Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].

Product Specifications

CAS Number

[866933-46-2]

Product Name Alternative

TD-5108

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/velusetrag.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC2=C(N(C(C)C)C1=O)C=CC=C2)N[C@@H]3C[C@@H](N4C[C@@H](O)CN(C)S(=O)(C)=O)CC[C@@H]4C3

Molecular Formula

C25H36N4O5S

Molecular Weight

504.64

References & Citations

[1]Smith JAM, et, al. The in vitro pharmacological profile of TD-5108, a selective 5-HT (4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378 (1) :125-37.|[2]Beattie DT, et, al. The in vivo gastrointestinal activity of TD-5108, a selective 5-HT (4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378 (1) :139-47.|[3]Ishii T, et, al. Serotonin 5-HT 4 Receptor Agonists Improve Facilitation of Contextual Fear Extinction in an MPTP-Induced Mouse Model of Parkinson's Disease. Int J Mol Sci. 2019 Oct 26;20 (21) :5340.|[4]Kuo B, et al. Velusetrag accelerates gastric emptying in subjects with gastroparesis: a multicentre, double-blind, randomised, placebo-controlled, phase 2 study. Aliment Pharmacol Ther. 2021;53 (10) :1090-1097.|[5]Goldberg M, et al. Clinical trial: the efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized, double-blind, placebo-controlled, dose-response study. Aliment Pharmacol Ther. 2010;32 (9) :1102-1112.