Lesopitron dihydrochloride

Name: Lesopitron dihydrochloride
Brand: TargetMol
SKU: T11839
Rating: 4.5 (1 reviews)

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Catalog No. T11839Cas No. 132449-89-9

Alias E4424

Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.

Lesopitron dihydrochloride

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Catalog No. T11839Alias E4424Cas No. 132449-89-9

Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	1-2 weeks	1-2 weeks
50 mg	$1,980	1-2 weeks	1-2 weeks
100 mg	$2,500	1-2 weeks	1-2 weeks

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

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Product Introduction

Bioactivity

Description	Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.
Targets&IC50	5-HT1A receptor:125 nM
In vitro	As expected of a full agonist at postsynaptic 5-HT1A receptors, Lesopitron (IC50=125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC50=120 nM)[1].In vitro binding and autoradiographic studies with [3H]8-OH-DPAT and [3H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT1A receptors in the rat brain with a relatively high affinity (pKi=7.35).
In vivo	Administering lesopitron at a dose known to elicit anxiolytic behavior in rats (30 μg/kg, i.p.) significantly decreases serotonin (5-HT) levels in cortical perfusates to 45% of the baseline. Additionally, lesopitron effectively suppresses the activity of serotoninergic neurons in live conditions, specifically in chloral hydrate-anesthetized rats, with an ID50 of 35 μg/kg when administered intravenously[1][2].
Synonyms	E4424

Chemical Properties

Molecular Weight	393.74
Formula	C₁₅H₂₃Cl₃N₆
Cas No.	132449-89-9
Smiles	Cl.Cl.Clc1cnn(CCCCN2CCN(CC2)c2ncccn2)c1
Relative Density.	1.31g/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.

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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.

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