ChemicalBook CAS DataBase List 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

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 Name4-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
CAS1142363-52-7
CBNumberCB23147155
MFC27H35N5O2
MW461.6
MDL NumberMFCD30489233
MOL File1142363-52-7.mol

Chemical Properties

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
FDA UNII	3NU609VYNF

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 Price

Product number	Packaging	Price	Product description	Buy
ChemScene CS-0039264	5mg	$210	Edicotinib 99.88%	Buy
Apolloscientific BISN0042	5mg	$264	JNJ-40346527	Buy
ChemScene CS-0039264	10mg	$350	Edicotinib 99.88%	Buy
Apolloscientific BISN0042	10mg	$426	JNJ-40346527	Buy
ChemScene CS-0039264	25mg	$750	Edicotinib 99.88%	Buy

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⁺CD11b^highLy6C^{intermediate/low}cells) 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 synthesis

Preparation Products And Raw materials

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

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32470	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
Nanjing Doge Biomedical Technology Co., Ltd	+86-25-58227606 +86-15305155328	sales@dogechemical.com	China	4128	58
HANGZHOU LEAP CHEM CO., LTD.	+86-571-87711850	market18@leapchem.com	China	24597	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8467	58
Suzhou ARTK Medchem Co., Ltd.	+86-512-68323658 +86-18168183658	sales1@artkmedchem.com	China	39002	58
Wuhan Jingkang en Biomedical Technology Co., Ltd	+8613720134139	orders@jknbiochem.com	China	5221	58
ZHENGZHOU JIUYI TIME NEW MATERIALS CO,.LTD	+86-13017695106 +86-13676922317	jiuyitime@fdachem.com	China	16513	58

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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 Spectrum

1142363-52-7, 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-carboxamideRelated Search

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