2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel MAPK/ERK Pathway NF-κB Immunology/Inflammation Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. 5-HT Receptor nAChR p38 MAPK NF-κB AP-1 Nuclear Factor of activated T Cells (NFAT) JAK
  4. Tropisetron

Tropisetron  (Synonyms: SDZ-ICS-930 free base)

Cat. No.: HY-B0072 Purity: 98.72%
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Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.

For research use only. We do not sell to patients.

Tropisetron Chemical Structure

Tropisetron Chemical Structure

CAS No. : 89565-68-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 32 In-stock
10 mg USD 50 In-stock
25 mg USD 90 In-stock
50 mg USD 160 In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of Tropisetron:

Tropisetron Related Antibodies

Top Publications Citing Use of Products

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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c-Fos c-Jun

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JAK1 JAK2 JAK3 Tyk2 JAK

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Description

Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects[1][2][3][4][5][6].

IC50 & Target

5-HT3 Receptor

5.3 nM (Ki)

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.

Tropisetron Related Antibodies

Western Blot Analysis[3]

Cell Line: LPS (HY-D1056) treated human monocytes
Concentration: 1, 10, 25 and 50 μg/mL
Incubation Time: 4 h
Result: Significantly reduced the activation of p38 MAPK.
Did not affect the expression of the non-phosphorylated form of p38 MAPK.
In Vivo

Tropisetron (2.5-7.5mg /kg; Intraperitoneal injection; 5 days) has an improved effect in a rat model of hemorrhagic cystitis induced by cyclophosphamide (HY-17420)[4].
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.

Animal Model: Cyclophosphamide (CTX) (HY-17420) treated adult female Sprague-Dawley (SD) rats (about 250 g)[4]
Dosage: 2.5, 5 and 7.5 mg/kg
Administration: Intraperitoneal injection (i.p.); 5 days
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.
Animal Model: BALB/c mouse with lung cancer[5]
Dosage: 5 mg/kg (22 days) and 10 mg/kg (10 days)
Administration: Intraperitoneal injection (i.p.)
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.
Animal Model: Male Wistar rats with chronic cerebral hypoperfusion (CCH)[6]
Dosage: 1 and 5 mg/kg
Administration: Intraperitoneal injection (i.p.); 35 days
Result: Ameliorated spatial memory impairment induced by CCH.
Restored neuronal count in the CA1 region, IL-6 serum level and SERT expression.
Clinical Trial
Molecular Weight

284.36

Formula

C17H20N2O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (11.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5167 mL 17.5834 mL 35.1668 mL
5 mM 0.7033 mL 3.5167 mL 7.0334 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5167 mL 17.5834 mL 35.1668 mL 87.9170 mL
5 mM 0.7033 mL 3.5167 mL 7.0334 mL 17.5834 mL
10 mM 0.3517 mL 1.7583 mL 3.5167 mL 8.7917 mL
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Tropisetron Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tropisetron89565-68-4SDZ-ICS-9305-HT ReceptornAChRp38 MAPKNF-κBAP-1Nuclear Factor of activated T Cells (NFAT)JAKSerotonin Receptor5-hydroxytryptamine ReceptorNicotinic acetylcholine receptorsNuclear factor-κBNuclear factor-kappaBActivator Protein 1Janus kinaseJurkatT cellsHuman monocytesHemorrhagic cystitis model Lung cancer model Spatial memory impairment modelInhibitorinhibitorinhibit

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