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BIA 10-2474

BIA 10-2474
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Purity:99.79%
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BIA 10-2474

Catalog No. T3354Cas 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.
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Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$47In Stock
10 mg$84In Stock
25 mg$158In Stock
50 mg$259In Stock
100 mg$413In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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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.
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].
AliasBIA10-2474
Chemical Properties
Molecular Weight300.36
FormulaC16H20N4O2
Cas No.1233855-46-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 4 mg/mL(13.3 mM)
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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