Tropisetron HCl

Catalog No.S1898 Synonyms: ICS 205-930

Tropisetron HCl Chemical Structure

Molecular Weight(MW): 320.81

Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
USD 670 In stock
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Biological Activity

Description Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.
Targets
5-HT3 [1]
In vitro

Tropisetron is a high affinity ligand for both th α7 nAChR and 5HT3R. Tropisetron has very low affinity for the other nicotinic subtypes tested. [1] Tropisetron is a potent and selective serotonin 3 (5-hydroxytryptamine3; 5-HT3) receptor antagonist with antiemetic properties, probably mediated via antagonism of receptors both at peripheral sites and in the central nervous system. [2] Tropisetron is a potent inhibitor of early and late events in TCR-mediated T cell activation. Tropisetron specifically inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Ttropisetron inhibits both the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation but in contrast TNF(alpha)-mediated NF-(kappa)B activation is not affected by this antagonist. [3] Tropisetron acts on α7 nAChRs on isolated pig retinal ganglion cells (RGCs) to provide neuroprotection against glutamate-induced excitotoxicity. Tropisetron acts to decrease p38MAP kinase levels to inhibit apoptosis. Tropisetron is able to protect retinal ganglion cells (RGCs) from a glutamate assault in a dose-dependent manner when applied to cultures 1 hour prior to glutamate application. [4]

In vivo Tropisetron (1 mg/kg i.p.) significantly improves the deficient inhibitory processing of the P20-N40 auditory evoked potential in DBA/2 mice. [5]

Protocol

Solubility (25°C)

In vitro Water 46 mg/mL (143.38 mM)
DMSO 35 mg/mL (109.09 mM)
Ethanol Insoluble

* 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 320.81
Formula

C17H20N2O2.HCl

CAS No. 105826-92-4
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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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID