产品描述:
BMS 986142 is a Bruton’s tyrosine kinase (BTK) inhibitor (IC50 = 0.5 nM).{61007} It is greater than 20-fold selective for BTK over a panel of 384 kinases. BMS 986142 inhibits calcium flux in Ramos B cells induced by B cell receptor (BCR) stimulation (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively). It inhibits TNF-α production in human peripheral blood mononuclear cells (PBMCs) induced by Fcγ receptor stimulation (IC50 = 3 nM). BMS 986142 (30 mg/kg per day) reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model. It reduces hind paw tibiotarsal joint bone resorption and inflammation in a mouse model of collagen antibody-induced arthritis (CAIA) when administered at doses of 5 and 20 mg/kg.{61000}