Home Tools

BIA 10-2474

Catalog No. T3354 CAS 1233855-46-3

Synonyms: 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BIA 10-2474, CAS 1233855-46-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 84.00
25 mg	In stock	$ 166.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 473.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

Bulk Inquiry

Select Batch

Purity: 99.79%

Biological Description

Chemical Properties

Storage & Solubility Information

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 proves to be a potent FAAH inhibitor with IC50s of 50-70 mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[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].

Synonyms	BIA10-2474
Molecular Weight	300.36
Formula	C16H20N4O2
CAS No.	1233855-46-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4 mg/mL(13.3 mM)

References and Literature

1. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20. 2. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial? Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library Anti-Obesity Compound Library Metabolism Compound Library Anti-Hypertension Compound Library Bioactive Compounds Library Max Bioactive Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

Dual FAAH/sEH-IN-1 MM-433593 CB2R/FAAH modulator-1 N-(3-Methoxybenzyl)Palmitamide SA 47 N-Benzyllinolenamide AM 374 N-Benzylpalmitamide

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

BIA 10-2474 1233855-46-3 Autophagy Metabolism Neuroscience FAAH BIA 10 2474 Fatty acid amide hydrolase Inhibitor BIA10-2474 BIA 102474 inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.