apj receptor agonist 1

APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research.

APJ receptor agonist 10 (Compound I choline salt) modulates the activity of the APJ receptor, making it useful for pulmonary hypertension research. Compared to its free form, this compound exhibits improved bioavailability.

Apelin agonist 1 is an orally available APJ receptor agonist with an EC50 value of 3.2 nM. Apelin agonist 1 is used in the study of cardiovascular disease.

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-36(rat, mouse) TFA, an endogenous agonist for the orphan G protein-coupled receptor APJ, exhibits a strong affinity for APJ receptors with an IC 50 of 5.4 nM and effectively inhibits cAMP production with an EC 50 of 0.52 nM. Moreover, it obstructs the invasion of certain HIV-1 and HIV-2 strains into NP-2 CD4 cells that express the APJ receptor [1] [2].

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ, demonstrating affinity for human APJ receptors on HEK 293 cells with a pIC50 value of 9.02. It also blocks the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells that express the APJ receptor [1] [2] [3].

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].

Endogenous APJ receptor agonist (EC50 = 20 nM) that is secreted by adipocytes. Binds with high affinity to human APJ receptors expressed in HEK 293 cells (pIC50= 8.61). Involved in regulation of cardiovascular function, fluid homeostasis and feeding. Bloc

Endogenous APJ receptor agonist that is secreted by adipocytes. Binds with high affinity to APJ receptors (IC50 = 5.4 nM) and potently inhibits cAMP production in vitro (EC50 = 0.52 nM). Involved in regulation of cardiovascular function, fluid homeostasis