RN 486
中文名称 | RN 486 |
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中文同义词 | 化合物RN486;化合物DBEQ;6-环丙基-8-氟-2-(2-(羟甲基)-3-(1-甲基-5-((5-(4-甲基哌嗪-1-基)吡啶-2-基)氨基)-6-氧代-1,6-二氢吡啶-3-基)苯基)异喹啉-1(2H)-酮 |
英文名称 | RN486 |
英文同义词 | RN486;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-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;RN486/RN-486;RN468;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;RN486 LM-2078;RN486 TFA Salt |
CAS号 | 1242156-23-5 |
分子式 | C35H35FN6O3 |
分子量 | 606.69 |
EINECS号 | 200-110-4 |
相关类别 | 小分子抑制剂;小分子抑制剂,天然产物;Inhibitors |
Mol文件 | 1242156-23-5.mol |
结构式 |
RN 486 性质
沸点 | 868.6±65.0 °C(Predicted) |
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密度 | 1.378±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | ≥30.35 mg/mL,溶于 DMSO,温和加热;不溶于水;不溶于乙醇 |
形态 | 固体 |
酸度系数(pKa) | 13.95±0.10(Predicted) |
颜色 | 米白色至浅黄色 |
CAS 数据库 | 1242156-23-5 |
RN486是一种有效的选择性BTK 抑制剂,IC50为4 nM。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.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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-18018 | RN 486 RN486 | 1242156-23-5 | 1mg | 679元 |
2024/08/19 | HY-18018 | RN 486 RN486 | 1242156-23-5 | 5mg | 1300元 |