4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide
- Product Name
- 4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide
- CAS No.
- 1142363-52-7
- Chemical Name
- 4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide
- Synonyms
- Edicotinib(JNJ-40346527);JNJ-40346527;CS-2865;JNJ-527;EDICOTINIB;JUJ-40346527;Edicotinib, 10 mM in DMSO;JNJ40346527; JNJ 40346527; JNJ-40346527; EDICOTINIB;5-Cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)-1H-imidazole-2-carboxamide;4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide
- CBNumber
- CB23147155
- Molecular Formula
- C27H35N5O2
- Formula Weight
- 461.6
- MOL File
- 1142363-52-7.mol
4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide Property
- Density
- 1.19±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:23.34(Max Conc. mg/mL);50.56(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.54(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);64.99(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);43.33(Max Conc. mM) - form
- A crystalline solid
- pka
- 13.82±0.70(Predicted)
- color
- White to off-white
- InChIKey
- BNVPFDRNGHMRJS-UHFFFAOYSA-N
- SMILES
- C1(C(NC2=CC=C(C3CC(C)(C)OC(C)(C)C3)N=C2C2CCC(C)(C)CC=2)=O)NC(C#N)=CN=1
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
- CS-0039264
- Product name
- Edicotinib
- Purity
- 99.88%
- Packaging
- 5mg
- Price
- $210
- Updated
- 2021/12/16
- Product number
- BISN0042
- Product name
- JNJ-40346527
- Packaging
- 5mg
- Price
- $264
- Updated
- 2021/12/16
- Product number
- CS-0039264
- Product name
- Edicotinib
- Purity
- 99.88%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- BISN0042
- Product name
- JNJ-40346527
- Packaging
- 10mg
- Price
- $426
- Updated
- 2021/12/16
- Product number
- CS-0039264
- Product name
- Edicotinib
- Purity
- 99.88%
- Packaging
- 25mg
- Price
- $750
- Updated
- 2021/12/16
4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide Chemical Properties,Usage,Production
Uses
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research[1][2].
in vivo
Edicotinib (oral gavage; 3, 10, 30 and 100 mg/kg; 5 days) significantly inhibits microglial proliferation in ME7 mice. It diminishes the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg, and JNJ-527 depletes up to 50% of patrolling blood monocytes at every dose tested (CD45+CD11bhighLy6Cintermediate/lowcells) with only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high cells) at 100 mg/kg[1].Edicotinib exhibits a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively[1].Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced,but not other inflammatory cytokines[1].
| Animal Model: | C57BL/6 J (Harlan) mice[1] |
| Dosage: | 3, 10, 30 and 100 mg/kg; 5 days |
| Administration: | Oral gavage |
| Result: | Did not affect microglial numbers when administered under 100 mg/kg. |
| Animal Model: | C57BL/6 J (Harlan) mice[1] |
| Dosage: | 30 mg/kg; 33 days |
| Administration: | Oral gavage |
| Result: | Limited microglial expansion and attenuated behavioural deficits in ME7-prion mice. |
References
[1] Mancuso R, et al. CSF1R?inhibitor?JNJ-40346527?attenuates?microglial?proliferation?and?neurodegeneration?in?P301S?mice.Brain.?2019 Oct 1;142(10):3243-3264. DOI:10.1093/brain/awz241
[2] Genovese MC, et al. Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.J Rheumatol. 2015 Oct;42(10):1752-60. DOI:10.3899/jrheum.141580
4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)- 1H-imidazole-2-carboxamide Suppliers
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