Tropisetron

Tropisetron is an orally active 5-HT3R antagonist (Ki = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC50 = 1.3 μM) . Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion[1][2][3][4][5][6].

Product Specifications

CAS Number

[89565-68-4]

Product Name Alternative

SDZ-ICS-930 (free base)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor; AP-1; JAK; nAChR; NF-κB; Nuclear Factor of activated T Cells (NFAT) ; p38 MAPK

Type

Reference compound

Related Pathways

Epigenetics; GPCR/G Protein; Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Assay Protocol

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

Concentration

10mM

Purity

99.93

Solubility

DMSO : < 1 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CNC2=C1C=CC=C2)O[C@H]3C[C@H]4CC[C@H](N4C)C3

Molecular Formula

C17H20N2O2

Molecular Weight

284.36

Precautions

H302, H315, H319, H335

References & Citations

[1]Macor JE, et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11 (3) :319-21.|[2]Vega Lde L, et al. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70 (3) :369-80.|[3]Stratz C, et al. The anti-inflammatory effects of the 5-HT? receptor antagonist tropisetron are mediated by the inhibition of p38 MAPK activation in primary human monocytes. Int Immunopharmacol. 2012 Aug;13 (4) :398-402.|[4]Guo L, et al. Tropisetron Ameliorated Cyclophosphamide-Induced Hemorrhagic Cystitis via Restraining TLR-4/NF-κB and JAK1/STAT3 Signaling Pathways. Arch Esp Urol. 2023 Feb;76 (1) :56-64.|[5]Rashidi M, et al. Tropisetron attenuates tumor growth and progression in an experimental model of mouse lung cancer. J Cell Biochem. 2020 Feb;121 (2) :1610-1622.|[6]Divanbeigi A, et al. Tropisetron But Not Granisetron Ameliorates Spatial Memory Impairment Induced by Chronic Cerebral Hypoperfusion. Neurochem Res. 2020 Nov;45 (11) :2631-2640.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

Lactoferrin

Citation 01

Acta Pharmacol Sin. 2024 Sep;45 (9) :1821-1831.|Drug Dev Res. 2024 Nov;85 (7) :e70002.|Int J Neuropsychopharmacol. 2019 Sep 1;22 (9) :574-584.|Cancer Lett. 2024 Aug 1:217150.