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)-
![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)- Structure](CAS/20210305/GIF/2247950-42-9.gif)
- CAS No.
- 2247950-42-9
- Chemical 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)-
- Synonyms
- IK-175;AHR antagonist 5 free base;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)-
- CBNumber:
- CB09787283
- Molecular Formula:
- C25H24FN7
- Molecular Weight:
- 441.5
- MDL Number:
- MOL File:
- 2247950-42-9.mol
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)- Chemical Properties,Uses,Production
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].
References
[1]. Marta Sanchez-Martin, et al. Ahr inhibitors and uses thereof. WO2021142180A1.
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)- Preparation Products And Raw materials
Raw materials
Preparation Products
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)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 999 | 58 |
| Jinan Jiuli Biotechnology Co. , Ltd. | 15865264761 | 486064515@qq.com | China | 3547 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62163 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24648 | 58 |
| Shanghai Tachizaki Biomedical Research Center | 18014399201 | sales@chemlab-tachizaki.com | China | 2560 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4870 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11974 | 58 |