g719x

Compound 40, NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal), a macrocyclic analogue of Ape13, acts as a potent APJ agonist with a Ki of 5.7 nM. It demonstrates favorable Gα12-biased signaling and possesses an enhanced in vivo half-life [1].

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.

Almonertinib hydrochloride (HS-10296 hydrochloride) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.