中文名 | RN486 |
英文名 | RN486 |
别名 | 化合物DBEQ 化合物RN486 |
英文别名 | RN468 RN486 RN 486 CS-689 RN-486 RN 486 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-yl)pyridin-2-yl)aMiNA)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquiNAlin-1(2H)-one 6-Cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-1(2H)-isoquinolinone |
CAS | 1242156-23-5 |
EINECS | 200-110-4 |
化学式 | C35H35FN6O3 |
分子量 | 606.69 |
密度 | 1.378±0.06 g/cm3(Predicted) |
沸点 | 868.6±65.0 °C(Predicted) |
溶解度 | DMSO: 24 mg/mL |
酸度系数 | 13.95±0.10(Predicted) |
存储条件 | -20℃ |
体外研究 | RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems. |
体内研究 | RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.648 ml | 8.241 ml | 16.483 ml |
5 mM | 0.33 ml | 1.648 ml | 3.297 ml |
10 mM | 0.165 ml | 0.824 ml | 1.648 ml |
5 mM | 0.033 ml | 0.165 ml | 0.33 ml |
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