Tropisetron

Catalog No.S5538 Synonyms: ICS 205-930

For research use only.

Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Tropisetron Chemical Structure

CAS No. 89565-68-4

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Biological Activity

Description Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
Targets
5-HT3 receptor [1]
()
α7 nAChR [1]
()
5.3 nM(Ki) 6.9 nM(Ki)
In vitro

Tropisetron inhibits antigen-induced proliferation and IL-2 production in human peripheral T cells. Tropisetron inhibits the signalling pathways that regulate the activation of the transcription factors NFAT, NF-κB and AP-1, which are known to play a critical role in the immune response[2].

In vivo Tropisetron could ameliorate the ischemic brain injury via decreasing myeloperoxidase activity and TNF-α level. Tropisetron elicits anti-inflammatory effects in experimental model of cisplatin-induced nephrotoxicity and these effects were completely 5-HT3-receptor-independent[3].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Jurkat cells
  • Concentrations: 10, 25, 50 μg/ml
  • Incubation Time: 30 min
  • Method:

    Jurkat cells (1 × 106 cells/ml) were stimulated with either TNFα (2 ng/ml) or PMA (20 ng/ml) plus ionomycin (0.5 ug/ml) for p65, JNK, ERK1 + 2, p38 and IκBα proteins in the presence or absence of tropisetron. Cells were then washed with PBS and proteins extracted in 50 μl of lysis buffer containing 0.5% NP-40. Protein concentration was determined by the Bradford assay and 30 μg of proteins were boiled in Laemmli buffer and electrophoresed in 10% SDS/polyacrylamide gels.

Animal Research:

[3]

  • Animal Models: Male albino mice
  • Dosages: 3 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Water 56 mg/mL
(196.94 mM)
DMSO 10 mg/mL
(35.16 mM)

Chemical Information

Molecular Weight 284.35
Formula

C17H20N2O2

CAS No. 89565-68-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04195204 Recruiting Drug: Tropisetron|Drug: Placebos Postoperative Cognitive Dysfunction|Postoperative Delirium Beijing Chao Yang Hospital November 1 2020 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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