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BIA 10-2474

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

Purity: 99.79%
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 SizePriceAvailabilityQuantity
5 mg$29In Stock
10 mg$48In Stock
25 mg$95In Stock
50 mg$155In Stock
100 mg$248In Stock
200 mg$368In Stock
1 mL x 10 mM (in DMSO)$32In Stock
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Purity:99.79%
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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].
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 | Shipping with blue ice.
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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