Home Tools

Lerisetron

Catalog No. T8441 CAS 143257-98-1

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Lerisetron, CAS 143257-98-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 75.00
2 mg	In stock	$ 98.00
5 mg	In stock	$ 153.00
10 mg	In stock	$ 232.00
25 mg	In stock	$ 411.00
50 mg	In stock	$ 597.00
100 mg	In stock	$ 868.00
1 mL * 10 mM (in DMSO)	In stock	$ 163.00

Bulk Inquiry

Select Batch

Purity: 99.15%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.
Targets&IC50	5-HT3 receptor (cell-free assay):0.81 μM
In vivo	showed a decrease in total clearance and distribution volume of the central compartment in old rats. The lerisetron free (unbound) fraction remained unchanged among the groups, and there were no significant differences in alpha(1)-acid glycoprotein levels. The concentration-effect relationship was best described by a sigmoid E(max) model. Since the drug concentration in plasma at half-maximal effect (EC(50)) decreased in old rats, an increased sensitivity to the effect of lerisetron in old animals could be expected.
Animal Research	Fischer 344 rats (n = 44) were divided into three groups, depending on their age: 5, 13, and 25 months. Blood samples were collected before administration of 200 micro g/kg of lerisetron for measurements of albumin, alpha(1)-acid glycoprotein, and unbound fraction of lerisetron. The lerisetron plasma concentrations were measured by high-performance liquid chromatography. A two-compartment model was fitted to the data using the nonlinear mixed-effects computer program WinNonMix. The population analysis was performed with the complete set of the collected data, and the potential sources of variability in the population parameters were investigated. Additionally, a pharmacodynamic study was performed. The effect of lerisetron (inhibition of the von Bezold-Jarisch reflex) was evaluated in young, adult, and senescent Fischer 344 rats.

Molecular Weight	292.38
Formula	C18H20N4
CAS No.	143257-98-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 53 mg/ml(181.27 mM)

References and Literature

1. Nerea, Jauregizar, Antonio, et al. Age-Related Changes in Pharmacokinetics and Pharmacodynamics of Lerisetron in the Rat: A Population Pharmacokinetic Model[J]. Gerontology, 2003. 2. Strenge H , Goebel S , Kowalski J , et al. Effects of Lerisetron, a New 5-HT3 Receptor Antagonist, on Ipecacuanha- induced Emesis in Healthy Volunteers[J]. Arzneimittelforschung, 2002, 52(09):689-694.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Serotonin Receptor-Targeted Compound Library Neuronal Signaling Compound Library Human Metabolite Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Angiogenesis related Compound Library Anti-Parkinson's Disease Compound Library

Related Products

Related compounds with same targets

Loxapine Palonosetron hydrochloride Molindone hydrochloride Jatrorrhizine chloride Zacopride hydrochloride Flopropione Thioridazine hydrochloride (R)-Mirtazapine D3

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Lerisetron 143257-98-1 GPCR/G Protein Neuroscience 5-HT Receptor Serotonin Receptor Serotonin Bradycardia Inhibitor 5-hydroxytryptamine Receptor Pharmacokinetics inhibit SD rats inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.