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ARN19702

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Catalog No. T9528Cas No. 1971937-18-4

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].

ARN19702

ARN19702

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Purity: 99.86%
Catalog No. T9528Cas No. 1971937-18-4
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$51In StockIn Stock
5 mg$122In StockIn Stock
10 mg$197In StockIn Stock
25 mg$389In StockIn Stock
50 mg$622In StockIn Stock
100 mg$978-In Stock
200 mg$1,320-In Stock
500 mg$1,96010-14 weeks10-14 weeks
1 mL x 10 mM (in DMSO)$133In StockIn Stock
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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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Purity:99.86%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].
Targets&IC50
NAAA:230 nM
In vivo
ARN19702, administered orally (po) at dosages of 3-10 mg/kg daily for seven consecutive days, effectively reduces Paclitaxel-induced neuropathic nociception in male rats without causing subacute antinociceptive tolerance [1]. In male mice, ARN19702 demonstrates a dose-dependent reduction in spontaneous nocifensive behaviors triggered by intraplantar formalin, and alleviates hypersensitivity following intraplantar carrageenan injection, paw incision, or sciatic nerve ligation, at dosages ranging from 0.1-30 mg/kg (po) [1]. Additionally, at a dosage range of 3-10 mg/kg (po), ARN19702 offers significant protection against multiple sclerosis in mice [2]. Pharmacokinetic analysis in mice reveals that at a 3 mg/kg dosage, ARN19702 achieves a maximum concentration (Cmax) of 1660±166 ng/mL and 613±68 ng/mL for intravenous (i.v.) and oral administration respectively, with corresponding times to reach Cmax (Tmax) of approximately 5.0 minutes (i.v.) and 30 minutes (po). The clearance (CL) rates stand at 33.2±1.6 mL/min/kg (i.v.) and 49±8 mL/min/kg (po), with half-lives (t 1/2) of 73.9±3.7 minutes (i.v.) and 104±16 minutes (po). Area under the curve (AUC) measurements indicate plasma levels of 1366.8±68.3 h×ng/mL (i.v.) and 988±157 h×ng/mL (po), and brain levels of 404.3±109.1 h×ng/mL (i.v.) and 181±28 h×ng/mL (po), with an oral bioavailability (F) of 72±11%.
Chemical Properties
Molecular Weight447.55
FormulaC21H22FN3O3S2
Cas No.1971937-18-4
SmilesCCS(=O)(=O)c1ccccc1C(=O)N1CCN(C[C@@H]1C)c1nc2ccc(F)cc2s1
Relative Density.1.359 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (111.72 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.47 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 mM2.2344 mL11.1719 mL22.3439 mL111.7194 mL
5 mM0.4469 mL2.2344 mL4.4688 mL22.3439 mL
10 mM0.2234 mL1.1172 mL2.2344 mL11.1719 mL
20 mM0.1117 mL0.5586 mL1.1172 mL5.5860 mL
50 mM0.0447 mL0.2234 mL0.4469 mL2.2344 mL
100 mM0.0223 mL0.1117 mL0.2234 mL1.1172 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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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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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