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EOS-62062

Name: EOS-62062
Brand: TargetMol
SKU: T4667
Rating: 4.5 (1 reviews)

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Catalog No. T4667Cas No. 1258963-59-5

Pesampator (PF-04958242) is a potent, highly selective positive allosteric modulator of the AMPA receptor, with an EC50 of 310 nM and a Ki of 170 nM, also known as an AMPA potentiator [1].

EOS-62062

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Catalog No. T4667Cas No. 1258963-59-5

Pesampator (PF-04958242) is a potent, highly selective positive allosteric modulator of the AMPA receptor, with an EC50 of 310 nM and a Ki of 170 nM, also known as an AMPA potentiator [1].

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Product Introduction

Bioactivity

Description

Pesampator (PF-04958242) is a potent, highly selective positive allosteric modulator of the AMPA receptor, with an EC50 of 310 nM and a Ki of 170 nM, also known as an AMPA potentiator [1].

In vivo

Pesampator administered subcutaneously (0.1-1 mg/kg) dose-dependently enhances cerebellum cGMP levels in CD-1 mice and at a dosage of 0.1-0.32 mg/kg, it shortens fall latency in C57BL/6J mice on an accelerating rotarod [1]. Furthermore, at dosages ranging from 0.001 to 0.01 mg/kg in male Sprague-Dawley rats, Pesampator counteracts the MK-801-induced (0.05 mg/kg; IV) decrease in paired-pulse facilitation (PPF) whether given cumulatively or as a single dose of 0.01 mg/kg intravenously [1]. At concentrations between 0.0032 and 0.032 mg/kg, it mitigates ketamine-caused disturbances in working memory in rats, evidenced by reduced errors in a radial arm maze [1]. Additionally, Pesampator exhibits a dose-dependent influence on the regional brain absorption of 2-deoxy-2-[18F]fluoro-D-glucose (FDG) in rats at dosages of 0.027, 0.08, and 0.60 mg/kg [1].

Chemical Properties

Molecular Weight	392.49
Formula	C₁₈H₂₀N₂O₄S₂
Cas No.	1258963-59-5
Smiles	CC(C)S(=O)(=O)N[C@H]1COC[C@H]1Oc1ccc(cc1)-c1ccc(s1)C#N
Relative Density.	1.37 g/cm3 (Predicted)

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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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