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Tropisetron HCl 5-HT Receptor antagonist

Name: Tropisetron HCl
Brand: Selleck Chemicals
SKU: S1898
Rating: 5 (1 reviews)

Cat.No.S1898

Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

Chemical Structure

Molecular Weight: 320.81

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other 5-HT Receptor Inhibitors	WAY-100635 Maleate Serotonin (5-HT) HCl Puerarin BRL-15572 Dihydrochloride SB269970 HCl Ketanserin RS-127445 Nuciferine Flopropione BRL-54443

Chemical Information, Storage & Stability

Molecular Weight	320.81	Formula	C₁₇H₂₀N₂O₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	105826-92-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ICS 205-930			Smiles	CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43.Cl

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (199.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 46 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-HT3
In vitro	Tropisetron is a high affinity ligand for both the α7 nAChR and 5HT3R. Tropisetron has very low affinity for the other nicotinic subtypes tested. 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. 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. Tropisetron 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. 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11212100/ [2] https://pubmed.ncbi.nlm.nih.gov/7507039/ [3] https://pubmed.ncbi.nlm.nih.gov/15922994/ [4] https://pubmed.ncbi.nlm.nih.gov/23727438/ [5] https://pubmed.ncbi.nlm.nih.gov/16136299/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04195204	Unknown status	Postoperative Cognitive Dysfunction\|Postoperative Delirium	Beijing Chao Yang Hospital	November 1 2020	Phase 4

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