BIA10-2474
- Product Name
- BIA10-2474
- CAS No.
- 1233855-46-3
- Chemical Name
- BIA10-2474
- Synonyms
- CS-2451;BIA10-2474;BIA 10-2474 ，S5932;BIA10-2474; BIA-10-2474;3-(1-(Cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide;1H-Imidazole-1-carboxamide,N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-;BIA 10 2474,Fatty acid amide hydrolase,FAAH,Autophagy,Inhibitor,BIA 102474,BIA 10-2474,inhibit
- CBNumber
- CB23159455
- Molecular Formula
- C16H20N4O2
- Formula Weight
- 300.36
- MOL File
- 1233855-46-3.mol
BIA10-2474 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:2.2(Max Conc. mg/mL);7.32(Max Conc. mM)
- form
- A crystalline solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 23157
- Product name
- BIA 10-2474
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $98
- Updated
- 2024/03/01
- Product number
- 23157
- Product name
- BIA 10-2474
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $177
- Updated
- 2024/03/01
- Product number
- 23157
- Product name
- BIA 10-2474
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $389
- Updated
- 2024/03/01
- Product number
- C987340
- Product name
- N-Cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
- Packaging
- 25mg
- Price
- $345
- Updated
- 2021/12/16
- Product number
- CS-6218
- Product name
- BIA10-2474
- Purity
- 98.41%
- Packaging
- 50mg
- Price
- $375
- Updated
- 2021/12/16
BIA10-2474 Chemical Properties,Usage,Production
Uses
N-Cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide is a potential fatty acid amide hydrolase (FAAH) inhibitor used for treating and preventing diseases.
Synthesis
1233855-18-9
1233855-46-3
In a further step of this synthesis, N-cyclohexyl-N-methyl-4-(pyridin-3-yl)-1H-imidazole-1-carboxamide (90 g, 317 mmol) was dissolved in dichloromethane (1350 ml) in a 2L reactor followed by addition of peracetic acid (84 ml, 475 mmol). The reaction mixture was stirred at 25 °C and the progress of the reaction was monitored by HPLC until N-cyclohexyl-N-methyl-4-(pyridin-3-yl)-1H-imidazole-1-carboxamide was completely consumed. After completion of the reaction, an aqueous solution (270 ml) of sodium metabisulfite (60.2 g, 317 mmol) was slowly added, keeping the reaction temperature below 30 °C. After performing phase separation, the organic phase was washed with water. After phase separation again, the organic phase was concentrated to 1/5 of the original volume at atmospheric pressure.Subsequently, the solvent was replaced with isopropanol (1350 ml) and the suspension was cooled down to 0 °C over a period of 4 hours and stirring was continued at this temperature for 1 hour. The resulting white crystalline solid was collected by filtration and washed sequentially with water (270 ml) and isopropanol (270 ml) to give 84.8 g (89% yield) of the target product.
in vivo
In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2].
References
[1] Patent: WO2012/15324, 2012, A1. Location in patent: Page/Page column 58-59
[2] Patent: US2012/65191, 2012, A1. Location in patent: Page/Page column 32
[3] Patent: WO2014/17938, 2014, A2. Location in patent: Page/Page column 67; 68
BIA10-2474 Preparation Products And Raw materials
Raw materials
Preparation Products
BIA10-2474 Suppliers
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View Lastest Price from BIA10-2474 manufacturers
- Product
- BIA10-2474 1233855-46-3
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 20kg
- Release date
- 2019-12-23