Tegaserod

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

Product Specifications

CAS Number

[145158-71-0]

UNSPSC

12352005

Hazard Statement

H317, H410

Target

5-HT Receptor; Apoptosis

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Metabolic Disease

Assay Protocol

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

Purity

99.89

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C16H23N5O

Molecular Weight

301.39

Precautions

H317, H410

References & Citations

[1]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.|[2]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.|[3]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.

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

Citation 01

Int Immunopharmacol. 2025 Sep 23:162:115181.|Nat Commun. 2025 Feb 7;16 (1) :1087.|Mol Med. 2025 Jan 29;31 (1) :30.

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