AT2R antagonist 1

Names

[ CAS No. ]:
2709031-17-2

[ Name ]:
AT2R antagonist 1

Biological Activity

[Description]:

AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common drug-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

[Target]

Ki: 29 nM (AT2R), 1000 nM (AT1R)[1]


[In Vitro]

AT2R antagonist 1 (compound 21) exhibits a negligible inhibition of CYP 3A (5%) and a very low tendency to inhibit CYP 2D6 (12%), 2C8 (26%), 2C9 (23%) and 2B6 (24%)[1].

[References]

[1]. Bolteau R, et al. Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine. Eur J Med Chem. 2020 Mar 1;189:112078.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H30N4O4S2

[ Molecular Weight ]:
490.64

Related Compounds

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