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Edicotinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Edicotinib图片
CAS NO:1142363-52-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight 461.61
Formula C27H35N5O2
CAS No. 1142363-52-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: N/A
Ethanol: N/A
Chemical Name4-Cyano-1H-imidazole-2-carboxylic acid N-(2-(4,4-dimethylcyclohex-1-enyl)-6-(2,2,6,6-tetramethyltetrahydropyran-4-yl)pyridin-3-yl)amide
SynonymsJNJ40346527; JNJ-527; JNJ 40346527; JNJ 527; JNJ-40346527; JNJ527; Edicotinib
实验参考方法
In Vitro

In vitro activity: Edicotinib, formerly known as JNJ-40346527, is a novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase. It is undergoing clinical investigation and acts to inhibit macrophage survival, proliferation, and differentiation in patients with active rheumatoid arthritis (RA) despite disease-modifying antirheumatic drug (DMARD) therapy. Pharmacokinetic exposure to JNJ-40346527 and its active metabolites was above the projected concentration needed for pharmacologic activity, and effective target engagement and proof of activity were demonstrated by increased levels of CSF-1 and decreased CD16+ monocytes in JNJ-40346527-treated, but not placebo-treated, patients. Thirty-seven (58.7%) JNJ-40346527-treated and 16 (50.0%) placebo-treated patients reported ≥ 1 adverse event (AE); 1 (1.6%) JNJ-40346527-treated and 3 (9.4%) placebo-treated patients reported ≥ 1 serious AE.


Kinase Assay: Edicotinib, formerly known as JNJ-40346527, is a novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase.

In VivoPharmacokinetic exposure to JNJ-40346527 and its active metabolites was above the projected concentration needed for pharmacologic activity, and effective target engagement and proof of activity were demonstrated by increased levels of CSF-1 and decreased CD16+ monocytes in JNJ-40346527-treated, but not placebo-treated, patients. Thirty-seven (58.7%) JNJ-40346527-treated and 16 (50.0%) placebo-treated patients reported ≥ 1 adverse event (AE); 1 (1.6%) JNJ-40346527-treated and 3 (9.4%) placebo-treated patients reported ≥ 1 serious AE. 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
Animal modelME7 mice
Formulation & DosageP.O.; 3, 10, 30 and 100 mg/kg
References J Rheumatol. 2015 Oct;42(10):1752-60; Brain. 2019 Oct 1;142(10):3243-3264.