Edicotinib
作者：齐岳
发布时间：2023-08-23
09:20:18
点击数：
产品名称：Edicotinib
产品描述：
| 产品描述 | Edicotinib is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment. | ||||||||||||||||
| 靶点活性 | FLT3:190 nM, Kit:20 nM , CSF-1R:3.2 nM | ||||||||||||||||
| 体外活性 | Edicotinib (0.1 nM-1μM; 24 hours) causes a dose-dependent decrease of CSF1R activation. Edicotinib (0.1 nM-1μM; 24 hours) lead to a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose-response curve displays the effect of Edicotinib on CSF1R and ERK1/2 (IC50: 18.6 nM and 22.5 nM for CSF1R and ERK1/2) [1].
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| 体内活性 | 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, however not other inflammatory cytokines. Edicotinib (oral gavage; 3, 10, 30, and 100 mg/kg; 5 days) obviously inhibits microglial proliferation in ME7 mice.?It reduces the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg. At every dose tested (CD45+CD11b high Ly6C intermediate/low cells), JNJ-527 depletes up to 50% of patrolling blood monocytes. Only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high?cells) at 100 mg/kg [1]. Edicotinib displays 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].
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| 别名 | JNJ-527, JNJ-40346527 |
| 分子量 | 461.61 |
| 分子式 | C27H35N5O2 |
| CAS No. | 1142363-52-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 15 mg/mL (32.4 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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