| Name | Edicotinib |
| Description | Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis. |
| In vitro | METHODS: N13 mouse microglial cell line was incubated with Edicotinib (JNJ-527) (0.1, 1, 10, 100, 1000 nM) for 30 min. We characterized the effects of the selective CSF1R inhibitor JNJ-527 on CSF1R activation in vitro. RESULTS Edicotinib (JNJ-527) resulted in a dose-dependent decrease in CSF1R activation and a reduction in ERK1 and ERK2 phosphorylation, with an IC50 of 18.6 nM for CSF1R and 22.5 nM for ERK1/2. [1] |
| In vivo | METHODS: ME7 mice were treated with JNJ-527 (3, 10, 30, 100 mg/kg, oral) for five consecutive days at 12 weeks post-induction (wpi), followed by a dose-response experiment to evaluate the potential of Edicotinib (JNJ-527) to block microglial proliferation in ME7-prion mice.
RESULTS Edicotinib (JNJ-527) administered at 30 mg/kg significantly blocked microglial proliferation in ME7-prion mice without altering the population dynamics in the healthy brain. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 2.31 mg/mL (5 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.17 mM), Sonication is recommended.
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| Keywords | rheumatoid | neurodegeneration | microglial | kit | JNJ527 | JNJ40346527 | JNJ 527 | JNJ 40346527 | Inhibitor | inhibit | FLT3 | expansion | Edicotinib | CSF-1R | CSF1R | CSF-1 receptor | colony stimulating factor 1 receptor | cKit | c-Fms | cFms | arthritis | alzheimer's disease |
| Inhibitors Related | Gilteritinib | Regorafenib monohydrate | Sunitinib | PLX5622 | Sorafenib | Dasatinib | Pexidartinib | Regorafenib | Brigatinib | Lenvatinib mesylate | Lenvatinib | Pazopanib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
