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BIA 10-2474

🥰Excellent
Catalog No. T3354Cas No. 1233855-46-3
Alias BIA10-2474

BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

BIA 10-2474

BIA 10-2474

🥰Excellent
Purity: 99.27%
Catalog No. T3354Alias BIA10-2474Cas No. 1233855-46-3
BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$34In StockIn Stock
25 mg$67In StockIn Stock
50 mg$109In StockIn Stock
100 mg$173In StockIn Stock
200 mg$258In StockIn Stock
1 mL x 10 mM (in DMSO)$29In 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:99.27%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.
Targets&IC50
FAAH (rat brain regions):50-70mg/kg (IC50)
In vitro
ExVivo: BIA 10-2474 is a potent FAAH inhibitor with IC50 values of 52 mg/kg (cerebellum), 67 mg/kg (rest of brain), 68 mg/kg (cortex), and 71 mg/kg (hypothalamus), and 50-70 mg/kg (i.p.) in various brain regions [1].
In vivo
In January 2016, a Phase I clinical trial involving the drug BIA 10-2474 experienced severe adverse events (SAE), including a fatality. Investigations into the trial's failure will explore various potential causes, such as off-target effects, miscalculated dosage, unforeseen immune responses, interspecies variability, and cumulative dose toxicity[2].
SynonymsBIA10-2474
Chemical Properties
Molecular Weight300.36
FormulaC16H20N4O2
Cas No.1233855-46-3
SmilesCN(C1CCCCC1)C(=O)n1cnc(c1)-c1ccc[n+]([O-])c1
Relative Density.no data available
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: 4 mg/mL (13.32 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3293 mL16.6467 mL33.2934 mL166.4669 mL
5 mM0.6659 mL3.3293 mL6.6587 mL33.2934 mL
10 mM0.3329 mL1.6647 mL3.3293 mL16.6467 mL

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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:
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:
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