Tropisetron

Catalog No.S5538 Synonyms: ICS 205-930

Tropisetron Chemical Structure

Molecular Weight(MW): 284.35

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

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Biological Activity

Description Tropisetron 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

Cell Research:

[2]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: Male albino mice
  • Formulation: normal saline
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 284.35
Formula

C17H20N2O2

CAS No. 89565-68-4
Storage powder
in solvent
Synonyms ICS 205-930

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02909478 Unknown status Chemotherapy-induced Nausea and Vomiting|Colorectal Cancer Sun Yat-sen University December 2016 Phase 3
NCT02909478 Unknown status Chemotherapy-induced Nausea and Vomiting|Colorectal Cancer Sun Yat-sen University December 2016 Phase 3
NCT02625181 Completed Postoperative Nausea and Vomiting Vanderbilt University|Vanderbilt University Medical Center July 2016 Not Applicable
NCT02625181 Completed Postoperative Nausea and Vomiting Vanderbilt University|Vanderbilt University Medical Center July 2016 Not Applicable
NCT02576327 Unknown status Vomiting Jun Zhu|Peking University October 2015 Phase 4
NCT02576327 Unknown status Vomiting Jun Zhu|Peking University October 2015 Phase 4

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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.

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID