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Lerisetron

Name: Lerisetron
Brand: TargetMol
SKU: T8441
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8441Cas No. 143257-98-1

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

Lerisetron

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Purity: 99.82%

Catalog No. T8441Cas No. 143257-98-1

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
5 mg	$129	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$348	In Stock	In Stock
50 mg	$513	In Stock	In Stock
100 mg	$737	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$123	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.82%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

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.

Chemical Properties

Molecular Weight	292.38
Formula	C₁₈H₂₀N₄
Cas No.	143257-98-1
Smiles	C(N1C(=NC=2C1=CC=CC2)N3CCNCC3)C4=CC=CC=C4
Relative Density.	1.22g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 53 mg/mL (181.27 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.84 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.4202 mL	17.1010 mL	34.2021 mL	171.0103 mL
5 mM	0.6840 mL	3.4202 mL	6.8404 mL	34.2021 mL
10 mM	0.3420 mL	1.7101 mL	3.4202 mL	17.1010 mL
20 mM	0.1710 mL	0.8551 mL	1.7101 mL	8.5505 mL
50 mM	0.0684 mL	0.3420 mL	0.6840 mL	3.4202 mL
100 mM	0.0342 mL	0.1710 mL	0.3420 mL	1.7101 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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