Product Details
| Product Name:
Edicotinib |
CAS No.:
1142363-52-7 |
| Purity:
99.69% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 1 mg/mL, Sonication is recommended.
|
| Keywords | CSF-1R | colony stimulating factor 1 receptor | CSF-1 receptor | JNJ40346527 | c-Fms | inhibit | Edicotinib | neurodegeneration | CSF1R | JNJ527 | Inhibitor | expansion | alzheimer’s disease | JNJ 527 | rheumatoid | microglial | JNJ 40346527 | arthritis |
| Inhibitors Related | Gilteritinib | Nintedanib | Regorafenib monohydrate | PLX5622 | Sorafenib | Pexidartinib | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate | Imatinib | Pazopanib | Axitinib |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease 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 | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$1980.00/50mg |
VIP1Y
|
TargetMol Chemicals Inc.
|
2024-10-22 |
United States