CAS:2162982-11-6(S)-6-(4-Chlorophenyl)-2-(3-fluorophenyl)-N-(1-hydroxypropan-2-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide

BAY-218 is an AHR antagonist.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

立即询价

实验数据

技术信息

CAS号

2162982-11-6

储存条件

分子式

C20H17ClFN3O3

运输

蓝冰

分子量

401.82

别名

溶解度

DMSO	150.0 mg/mL (373.3 mM)
Water	insoluble

动物实验配方

生物活性

描述The aryl hydrocarbon receptor is an important transcription factor involved in immunosuppression. BAY-218 is a selective, potent, small-molecule inhibitor of AhR. It inhibits the nuclear translocation of AhR, the expression of dioxin response element (DRE)-luciferase reporter and the expression of genes regulated by AhR. In LPS-treated primary human monocytes, BAY-218 rescued KA-suppressed TNF-α production. BAY-218 also increased the expression of T cell cytokine in a human mixed lymphocyte reaction and a mouse antigen-specific bone-marrow-derived dendritic cell-OT-I T cell co-culture. In vivo, BAY-218 promoted immune responses against tumor cells and suppressed tumor growth in the syngeneic mouse models of CT26 and B16-OVA. BAY-218 treatment elevated the frequency of tumor-infiltrating CD8+ T cells and NK cells, whereas the frequency of GR1+ myeloid cells and CD206+M2 macrophages was decreased. An enhanced therapeutic efficacy was observed in anti-PD-L1 antibody-treated CT26 model with the presence of BAY-218.
作用机制BAY-218 is a novel AhR inhibitor that inhibits AhR nuclear translocation.