1559069-92-9
Chemical Structure
Edicotinib hydrochloride
Synonym(s): JNJ-40346527 hydrochloride; JNJ-527 hydrochloride
- CAS No.: 1559069-92-9
- Formula:C27H36ClN5O2
- Molecular Weight:498.06
InChIKey: GDFIUUZLRLJTSJ-UHFFFAOYSA-N
SMILES: O=C(C1=NC=C(C#N)N1)NC2=C(C3=CCC(C)(C)CC3)N=C(C(CC(C)(C)O4)CC4(C)C)C=C2.Cl
Biological Activity: Edicotinib hydrochloride 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 hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research[1][2].
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Edicotinib hydrochloride | Edicotinib hydrochloride 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 hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
