AHR antagonist 5 free base

Research use only, not for human use.

AHR antagonist 5 free base is an orally active AHR antagonist with IC50 of approximately 35-150 nM in human and rodent cell lines, and exhibits anticancer activity.

AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.

AHR antagonist 5 free base (Compound A) potently inhibits AHR activity in human and rodent cell lines (IC50 of ~35-150 nM). In human T cell assays, AHR antagonist 5 free base induces an activated T cell state. AHR antagonist 5 free base inhibits CYP1A1 and interleukin (IL)-22 gene expression and leads to an increase in pro-inflammatory cytokines, such as IL-2 and IL-9.

AHR antagonist 5 free base (Compound A) has been evaluated in a series of pharmacological, single-dose and repeated-dose toxicological studies in rodent and non-rodent species including 28-day Good Laboratory Practice (GLP) studies in rat and monkeys. All changes are resolved or resolving after 2 weeks of dosing cessation, except for the testicular changes in rats.

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Others

Other Targets

Aryl Hydrocarbon Receptor

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2247950-42-9

441.5

C25H24FN7

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (226.50 mM; Ultrasonic )

N(C=1N2C(=C(C(C)C)C=N2)N=C(N1)C=3C=C(F)C=NC3)[C@H]4CC=5C=6C(NC5CC4)=CC=CC6

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(-20℃)

With Ice Pack

≥ 2 years