AT2R antagonist 1

Modify Date: 2024-01-02 16:21:57

AT2R antagonist 1 Structure
AT2R antagonist 1 structure
Common Name AT2R antagonist 1
CAS Number 2709031-17-2 Molecular Weight 490.64
Density N/A Boiling Point N/A
Molecular Formula C23H30N4O4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AT2R antagonist 1


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].

 Names

Name AT2R antagonist 1

 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
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