ahr antagonist 5

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.

AHR antagonist 5 free base 是一种具有口服活性的 AHR 拮抗剂，在人和啮齿动物细胞系中的 IC50 约为 35-150 nM,具有抗癌活性。

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。

AHR-16303B oxalate is a novel antagonist of 5-HT2 receptors.

CHD-5 is a selective antagonist of the aryl hydrocarbon receptor (AhR).

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.