化合物BMS-935177 T14681

Product Introduction
Bioactivity


英文名: BMS-935177

描述: BMS-935177 是一种可逆的 BTK 抑制剂，IC50 值为 3 nM。

体外活性: In human Ramos B cells, BMS-935177 inhibits calcium flux with an IC50 of 27 nM. BMS-935177 inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. Against IgG-containing immune complexdriven low affinity activating FcγRIIa and FcγRIII end points in peripheral blood mononuclear cells, BMS-935177 effectively inhibits TNFα production (IC50 = 14 nM). BMS-935177 shows mean IC50 values of 550 and 2060 nM in human and mouse whole blood, respectively[1].

体内活性: BMS-935177(5, 20, and 45 mg/kg) inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice, BMS-935177 (5 mg/kg) maintains the plasma concentration above the mouse whole blood BCR-stimulated CD69 IC50 value of 2 μM for only 5 h. BMS-935177(10, 20, and 30 mg/kg) provides dose-dependently reduces both the severity and incidence of clinically evident disease in this rodent model of RA. BMS-935177(10 mg/kg) reduces the disease severity about 40%, and the percentage of animals showing any signs of disease is reduced by a third[1].

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 117mg/mL (232.8mM)


关键字: BMS935177 | BMS-935177 | BMS 935177

相关产品: Ibrutinib deacryloylpiperidine | JDB175 | JAK3/BTK-IN-2 | Cinsebrutinib | Tirabrutinib hydrochloride | CP-547632 | Tilfrinib | PCI-33380 | (±)-Zanubrutinib | Vecabrutinib

化合物BMS-935177 T14681信息由TargetMol中国为您提供，如您想了解更多关于化合物BMS-935177 T14681报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途