Tegaserod (maleate)

Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research[1][2][3].

Product Specifications

CAS Number

[189188-57-6]

Product Name Alternative

SDZ-HTF-919; HTF-919

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor; Apoptosis

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Tegaserod-maleate.html

Concentration

10mM

Purity

99.90

Solubility

DMSO : ≥ 35 mg/mL|H2O : < 0.1 mg/mL

Smiles

O=C(O)/C=C\C(O)=O.COC1=CC=C(NC=C2/C=N/NC(NCCCCC)=N)C2=C1

Molecular Formula

C20H27N5O5

Molecular Weight

417.46

Precautions

H302, H315, H319, H335

References & Citations

[1]M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17 (5) :738-43.|[2]D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143 (5) :549-60.|[3]Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39 (1) :38.