human apelin receptor

CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.

ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide.

Apelin-17 (human, bovine) acetate is an endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94).

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.

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-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].

ELA-32(human) TFA is a potent apelin receptor agonist with high affinity, demonstrating an IC50 of 0.27 nM and a Kd of 0.51 nM. This compound does not bind to GPR15 or GPR25. It activates the PI3K/AKT signaling pathway, facilitating self-renewal of human embryonic stem cells (hESCs) through cell-cycle progression and protein synthesis. Additionally, ELA-32(human) TFA enhances the TGFβ pathway, predisposing hESCs towards an endoderm lineage, and promotes angiogenesis in HUVEC cells.

ELA-11(human) TFA, a bioactive fragment of ELA-32, acts as a high-affinity apelin receptor agonist (K i =14 nM). It effectively inhibits forskolin-induced cAMP production and promotes β-arrestin recruitment in vitro, highlighting its significant agonistic activity.

ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

Apelin-16, human, bovine acetate, is a bioactive peptide. (Apelin is the endogenous ligand for the G protein-coupled APJ receptor. It is derived from a 77-amino acid precursor protein. Apelin-16 represents one of the active fragments of Apelin).