aladdin 阿拉丁 R413708 RN486 1242156-23-5 98%

中文名：RN486

英文名：RN486

纯度：Moligand™，≥98%

货号：R413708

Cas号：1242156-23-5

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

RN486 RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.

Targets

BTK 4 nM

In vitro

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.

In vivo

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.

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