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AM-2099

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Catalog No. T14201Cas No. 1443373-17-8
Alias AM2099

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

AM-2099

AM-2099

😃Good
Catalog No. T14201Alias AM2099Cas No. 1443373-17-8
AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$2995 days5 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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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Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.
Targets&IC50
Nav1.7 (rat):3.5 μM, Nav1.7 (human):0.16 μM, Nav1.7 (mouse):0.18 μM
In vitro
AM-2099 is more than 100-fold selective over Nav1.3, Nav1.4, Nav1.5, and Nav1.8, while lower levels of selectivity are observed against Nav1.1, Nav1.2, and Nav1.6. AM-2099 demonstrates low affinity for hERG (>30 µM) and does not show greater than 50% inhibition against a panel of 100 kinases (1 µM) and a broad CEREP panel (10 µM). In heterologous cells, comparable inhibition is observed across human, mouse, dog, and cynomolgus monkey NaV1.7 with reduced activity against rat NaV1.7.[1]
In vivo
AM-2099 demonstrates a dose-dependent increase in plasma exposure with a concomitant dose-dependent reduction in scratching bouts compared to vehicle-treated animals, with a statistically significant reduction observed at the 60 mg/kg dose.
AM-2099 demonstrates a favorable pharmacokinetic profile in rat and dog. In rats AM-2099 shows low total clearance and moderate Vdss and half-life. However, when dosed in dogs AM-2099 shows very low clearance, a low Vdss and long halflife (18 h).[1]
SynonymsAM2099
Chemical Properties
Molecular Weight466.46
FormulaC19H13F3N4O3S2
Cas No.1443373-17-8
SmilesO=S(=O)(NC1=NC=CS1)C=2C=CC=3C(=NC=NC3C=4C=CC(=CC4OC)C(F)(F)F)C2
Relative Density.1.531 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: 120 mg/mL (257.26 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.07 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
1mg5mg10mg50mg
1 mM2.1438 mL10.7190 mL21.4381 mL107.1903 mL
5 mM0.4288 mL2.1438 mL4.2876 mL21.4381 mL
10 mM0.2144 mL1.0719 mL2.1438 mL10.7190 mL
20 mM0.1072 mL0.5360 mL1.0719 mL5.3595 mL
50 mM0.0429 mL0.2144 mL0.4288 mL2.1438 mL
100 mM0.0214 mL0.1072 mL0.2144 mL1.0719 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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