Buying Guide,is an apelin receptor agonist

Azelaprag, also known by its development code AMG 986, is a groundbreaking peptide that functions as a potent and selective apelin receptor (APJ) agonist. This small-molecule agonist has garnered significant attention for its potential therapeutic applications, particularly in the realm of cardiovascular diseases and muscle-related conditions. The search keyword "amg 986 peptide" leads to a wealth of information highlighting its pharmacological properties, clinical development, and the entities involved in its research and potential commercialization.

At its core, AMG 986 targets the apelin receptor (APJ), a G protein-coupled receptor that binds to peptide hormones known as apelins (APLN). The interaction of Azelaprag with the APJ receptor leads to a cascade of downstream effects, including improved cardiac contractility. This mechanism of action is a key aspect of its development for conditions like heart failure. Research indicates that Azelaprag exhibits a high affinity for the APJ receptor, with an EC50 of 0.32 nM, signifying its potency. Furthermore, studies have shown that AMG 986 improves cardiac contractility in animal models without causing adverse hemodynamic impacts.

The development journey of AMG 986 has involved several key players and stages. Initially developed by Amgen, it was later licensed to BioAge Labs and subsequently renamed BGE-105. This transition highlights the collaborative nature of drug discovery and development. The compound has been explored through various clinical trials, including a first-in-human study designed to evaluate its safety and tolerability. These studies have included both healthy subjects and patients with heart failure (HF). Some research suggests that AMG 986 treatment was well tolerated in healthy subjects and demonstrated positive changes in ejection fraction and stroke volume in HF patients.

Beyond cardiovascular applications, Azelaprag has also shown promise in addressing muscle-related issues. BioAge Labs is particularly interested in its potential for targeting muscle aging. BGE-105 (formerly AMG 986) mimics the production of apelin, a peptide that has demonstrated benefits in muscle regeneration in animal studies. This suggests a broader therapeutic spectrum for the AMG 986 peptide.

The chemical identity of Azelaprag is also well-documented. Its CAS number is 2049980-18-7. It is described as a candidate active molecule and an apelin receptor agonist agent candidate. The molecular weight is reported as 523.61, with a chemical formula of C25H29N7O4S. The compound can be administered orally or intravenously, adding to its versatility in potential treatment regimens.

The development of AMG 986 represents a significant advancement in targeting the apelin receptor. Its ability to act as a potent agonist and its potential to treat conditions such as heart failure (HF), as well as neurological and cardiovascular diseases, underscore its therapeutic value. Further research and clinical evaluations are currently underway evaluating AMG 986, aiming to fully unlock its potential as a candidat for various medical conditions. The exploration of Azelaprag (AMG 986), including its pharmacokinetics and safety, continues to be a focal point in pharmaceutical research.