RN-486

A potent and selective BTK inhibitor with IC50 of 4 nM in the enzymatic assay; shows high selectivity against a panel of 369 kinases; blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50=2.9 nM) and Fcγ receptor engagement-mediated TNFα production in monocytes (IC50=7.0 nM) ; robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models.Rheumatoid Arthritis Preclinical (In Vitro) :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. (In Vivo) :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.

1242156-23-5

RN 486 | RN486

>98% (HPLC)

DMSO: 24 mg/mL

CN1CCN (CC1) C1=CN=C (NC2=CC (=CN (C) C2=O) C2=C (CO) C (=CC=C2) N2C=CC3=CC (=CC (F) =C3C2=O) C2CC2) C=C1

C35H35FN6O3

606.6892

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.