Tropisetron
Based on 5 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.93%
- CAS No.: 89565-68-4
- Formule: C17H20N2O2
- Masse moléculaire:284.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tropisetron
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Activité biologique
Description
IC50 & Target
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5-HT3 Receptor 5.3 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Oocyte | EC50 |
10 nM
Compound: Tropisetron ICS-205-930
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Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
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[PMID: 15050614] |
| Oocyte | IC50 |
1.8 μM
Compound: Tropisetron ICS-205-930
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Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes
Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes
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[PMID: 15050614] |
| Oocyte | IC50 |
170 μM
Compound: Tropisetron ICS-205-930
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Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes
Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes
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[PMID: 15050614] |
In Vitro
ropisetron (10-50 μg/mL; 72 h) inhibits T cell activation in human peripheral T cells[2].
Tropisetron (10-50 μg/mL; 30 min) inhibits the activation of NFAT, AP-1, NF-κB and IL-2 production in Jurkat cells[2].
Tropisetron (1-50 μg/mL; 4 h) decreases the phosphorylation level of p38 MAPK in human monocytes treated with LPS (HY-D1056)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LPS (HY-D1056) treated human monocytes
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Concentration:1, 10, 25 and 50 μg/mL
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Incubation Time:4 h
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Result:Significantly reduced the activation of p38 MAPK.
Did not affect the expression of the non-phosphorylated form of p38 MAPK.
In Vivo
Tropisetron (5-10 mg/kg; Intraperitoneal injection; 10-22 days) has antitumor effect in lung cancer mouse model[5].
Tropisetron (1-5 mg/kg; Intraperitoneal injection; 35 days) improves the spatial memory impairment induced by chronic cerebral hypoperfusion in rat models[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cyclophosphamide (CTX) (HY-17420) treated adult female Sprague-Dawley (SD) rats (about 250 g)[4]
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Dosage:2.5, 5 and 7.5 mg/kg
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Administration:Intraperitoneal injection (i.p.); 5 days
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Result:Restrained apoptosis in kidney cells.
Alleviated oxidative stress and inflammatory damage.
Ameliorated CTX-induced cystitis by restraining TLR-4/NF-κB and JAK1/STAT3 signalling pathways.
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Animal Model:BALB/c mouse with lung cancer[5]
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Dosage:5 mg/kg (22 days) and 10 mg/kg (10 days)
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Administration:Intraperitoneal injection (i.p.)
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Result:Showed significantly lower tumor sizes at the day 24th after tumor induction.
Increased the levels of IFN-γ, E-cadherin, pathologic response, and necrotic cells and reduced the levels of IL-4 and Ki-67.
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Animal Model:Male Wistar rats with chronic cerebral hypoperfusion (CCH)[6]
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Dosage:1 and 5 mg/kg
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Administration:Intraperitoneal injection (i.p.); 35 days
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Result:Ameliorated spatial memory impairment induced by CCH.
Restored neuronal count in the CA1 region, IL-6 serum level and SERT expression.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 89565-68-4
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Appearance Solid
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Masse moléculaire 284.36
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Formule C17H20N2O2
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Color White to light yellow
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SMILES
O=C(C1=CNC2=C1C=CC=C2)O[C@H]3C[C@H]4CC[C@H](N4C)C3
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Synonyms
SDZ-ICS-930 free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Lett
Serotonylation in tumor-associated fibroblasts contributes to the tumor-promoting roles of serotonin in colorectal cancer. [Abstract]2024 Sep 28:600:217150. PMID: 39097134 -
Acta Pharmacol Sin
Sodium oligomannate activates the enteroendocrine-vagal afferent pathways in APP/PS1 mice. [Abstract]2024 Sep;45(9):1821-1831. PMID: 38702501 -
Int J Neuropsychopharmacol
2019 Sep 1;22(9):574-584. PMID: 31125405 -
Drug Dev Res
Tropisetron attenuates high glucose-induced oxidative stress and inflammation in ARPE-19 cells in vitro via regulating SIRT1/ROCK1 signaling. [Abstract]2024 Nov;85(7):e70002. PMID: 39381984 -
Virus Res
Ondansetron exhibits potent antiviral activity against enterovirus 71 infection in vitro and in vivo. [Abstract]2026 Jun 25:370:199771. PMID: 42349797
Solvant et solubilité
In Vitro:
DMSO : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 0.1 mg/mL (insoluble)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (9.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (9.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 46.67 mg/mL (164.12 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (284 KB)
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SDS (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tropisetron Related Classifications
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