| Bioactivity | 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]. |
| Target | Ki: 29 nM (AT2R), 1000 nM (AT1R) |
| Invitro | 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]. |
| Name | AT2R antagonist 1 |
| CAS | 2709031-17-2 |
| Formula | C23H30N4O4S2 |
| Molar Mass | 490.64 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
AT2R antagonist 1
CAS: 2709031-17-2 F: C23H30N4O4S2 W: 490.64
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonis
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