| Identification | Back Directory | [Name]
1H-Carbazol-3-amine, N-[2-(5-fluoro-3-pyridinyl)-8-(1-methylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]-2,3,4,9-tetrahydro-, (3R)- | [CAS]
2247950-42-9 | [Synonyms]
1H-Carbazol-3-amine, N-[2-(5-fluoro-3-pyridinyl)-8-(1-methylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]-2,3,4,9-tetrahydro-, (3R)- | [Molecular Formula]
C25H24FN7 | [MOL File]
2247950-42-9.mol | [Molecular Weight]
441.5 |
| Hazard Information | Back Directory | [Biological 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[1].
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[1].
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[1]. | [storage]
Store at -20°C | [References]
[1]. Marta Sanchez-Martin, et al. Ahr inhibitors and uses thereof. WO2021142180A1. |
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