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Velusetrag

CAT: 0804-HY-10457-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10457-01Size:5 mg
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
5-HT2 Receptor; Apolipoprotein D

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BA5019-10Velusetrag
RJB93351-01Velusetrag hydrochloride

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