ahr antagonist-1

Bindarit (AF2838)是一种芳基烃受体(AHR)拮抗剂，在人胶质母细胞瘤U87细胞系中的IC50值为 39.9 nM。BAY-218 抑制 AhR 在体外刺激促炎单核细胞和 T 细胞反应，并驱动抗肿瘤免疫反应，导致体内肿瘤生长减少。

AHR antagonist 5 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 39; IC50 < 0.5 μΜ). It significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.

PDM11 (1-[2-(4-Chloro-phenyl)-vinyl]-3,5-diMeth) 是抗氧化剂白藜芦醇的衍生物。它在白藜芦醇活性测定中不活跃。它对辐射分解产生的羟基自由基引发的亚油酸胶束氧化没有明显的保护作用。

AHR antagonist 5 hemimaleate 是一种口服具有活力的芳香烃受体 (AHR) 的有效拮抗剂 (IC50< 0.5 μM)。AHR antagonist 5 hemimaleate 联合检测点抑制剂 anti-PD-1 对肿瘤生长表现出抑制作用。

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

CB7993113是一种有效的AHR拮抗剂，IC50为0.33 μM。CB7993113直接结合AHR蛋白并阻断AHR核转位，可分别抑制多环芳烃(PAH)和TCDD诱导的报告基因活性75%和90%。

WAY-605471是一种 AHR 拮抗剂，IC50为0.5 - 1 μM。