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AMPA receptor modulator-1

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Catalog No. T10307Cas No. 2036074-41-4

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

AMPA receptor modulator-1

AMPA receptor modulator-1

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Purity: 99.93%
Catalog No. T10307Cas No. 2036074-41-4
AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$117In StockIn Stock
5 mg$268In StockIn Stock
10 mg$394-In Stock
25 mg$592-In Stock
50 mg$828-In Stock
100 mg$1,130-In Stock
1 mL x 10 mM (in DMSO)$271In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.93%
Appearance:Solid
Color:Purple
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Product Introduction

AMPA receptor modulator-1 AI Summary
AMPA receptor modulator-1 exhibits potent activity in blocking glutamate-induced calcium flux via the GluA1 flop isoform/TARPgamma8 receptor with an IC50 of 0.1995 nM, while showing much lower activity against the same receptor isoform with TARPgamma2, with an IC50 of 10,000.0 nM. This compound shows moderate to high clearance and a half-life of 1.9 hours in Sprague-Dawley rats, along with moderate hepatic extraction ratios in both human and rat liver microsomes. It has good solubility in simulated gastric fluid, but significantly higher solubility in fasted state simulated intestinal fluid. AMPA receptor modulator-1 demonstrates moderate protein binding in both human and rat plasma, with slightly higher binding in rat plasma. It displays potent ex vivo receptor occupancy at GluA/TARPgamma8 receptors in rats, resulting in a reduction in receptor labeling in the hippocampus at specific concentrations. Additionally, it shows good selectivity for the GluA1 flop isoform/TARPgamma8 receptor over the GluA1 flop isoform/TARPgamma2 receptor and has a moderate volume of distribution at steady state in Sprague-Dawley rats..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.
Targets&IC50
TARPγ 8:9.7
Chemical Properties
Molecular Weight341.71
FormulaC16H11ClF3NO2
Cas No.2036074-41-4
SmilesO(C(F)(F)F)C1=C(C=2C=C3C(=C(C)C2)NC(=O)C3)C(Cl)=CC=C1
Relative Density.1.394 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 3.42 mg/mL (10.01 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9265 mL14.6323 mL29.2646 mL146.3229 mL
5 mM0.5853 mL2.9265 mL5.8529 mL29.2646 mL
10 mM0.2926 mL1.4632 mL2.9265 mL14.6323 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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