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Velusetrag
$350 – $1,800
Products Details
Product Description
– 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].
Web ID
– HY-10457
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C25H36N4O5S
References
– [1]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.|[2]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.|[3]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.|[4]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.|[5]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.
CAS Number
– 866933-46-2
Molecular Weight
– 504.64
Compound Purity
– 99.64
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
Clinical Information
– Launched
Research Area
– Metabolic Disease; Neurological Disease
Solubility
– DMSO : 100 mg/mL (ultrasonic)
Target
– 5-HT Receptor
Isoform
– 5-HT4 Receptor
Pathway
– GPCR/G Protein;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
