RN 486 CAS#: 1242156-23-5

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RN 486

生物活性体外研究体内研究 用途与合成方法 MSDS RN 486价格(试剂级) 上下游产品信息

中文名称	RN 486
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;CS-689;RN486; RN-486; RN 486;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
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

RN 486 用途与合成方法

生物活性

RN486是一种有效的选择性BTK 抑制剂，IC50为4 nM。

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.

安全信息

MSDS信息

RN 486 价格(试剂级)

RN 486 上下游产品信息