2247950-42-9
2247950-42-9 structure
- Name: AHR antagonist 5 free base
- Chemical Name: AHR antagonist 5 free base
- CAS Number: 2247950-42-9
- Molecular Formula: C25H24FN7
- Molecular Weight: 441.50
- Catalog: Signaling Pathways Immunology/Inflammation Aryl Hydrocarbon Receptor
- Create Date: 2021-09-06 09:11:37
- Modify Date: 2024-01-07 23:00:59
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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].
| Name | AHR antagonist 5 free base |
|---|
| Description | 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]. |
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| Related Catalog | |
| In Vitro | 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]. |
| In Vivo | 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]. |
| References |
[1]. Marta Sanchez-Martin, et al. Ahr inhibitors and uses thereof. WO2021142180A1. |
| Molecular Formula | C25H24FN7 |
|---|---|
| Molecular Weight | 441.50 |