RN-486

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 BTK 抑制剂，酶测定中 IC50 为 4 nM；对一组 369 种激酶表现出高选择性；阻断肥大细胞中 Fcε 受体交联诱导的脱粒 (IC50=2.9 nM) 和单核细胞中 Fcγ 受体接合介导的 TNFα 产生 (IC50=7.0 nM)；在小鼠 CIA 和大鼠佐剂诱导关节炎 (AIA) 模型中具有强大的抗炎和骨保护作用。

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.

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.

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.

RN 486 | RN486

Tyrosine Kinase

BTK

BTK

Inflammation/Immunology

Rheumatoid Arthritis

1242156-23-5

606.6892

C35H35FN6O3

>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

1(2H)-Isoquinolinone, 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-

(-20℃)

With Ice Pack

≥ 2 years