RN486 是一种有效的，选择性的，具有口服活性的 Btk 抑制剂，IC₅₀ 为 4.0 nM，K_d 为 0.31 nM，对其他激酶的活性较低。RN486 可用于类风湿关节炎和系统性红斑狼疮的研究。

RN486 is a potent, selective and orally active Btk inhibitor with an IC 50 of 4.0 nM and a K d of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.

Solid

IC50: 4.0 nM (Btk)
Kd: 0.31 nM (Btk)

RN486 blocks 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 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM).
In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486. has not independently confirmed the accuracy of these methods. They are for reference only.

RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Xu D, et al. RN486, a selective Brutons tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.
[2]. Hsu J, et al. Brutons Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104.

In Vitro: DMSO : 24 mg/mL (39.56 mM; Need ultrasonic and warming)配制储备液