| Description |
[Pyr1]apelin-13 (human) (CAS: 217082-60-5)
Apelin GPCR-Receptor
The Apelin receptor, also known as APJ, APLNR, and AGTRL1, is a member of the class A family of G protein-coupled receptors (GPCRs). It has been identified in various species, including mouse, rat, cow, rhesus macaque, Xenopus laevis, and Danio rerio, and it shares structural similarities with the angiotensin II type l receptor (AT1). However, despite a 54% homology in transmembrane regions with AT1, it does not bind angiotensin II.
Initially designated as an "orphan" GPCR, due to the absence of a known ligand, O'Dowd & al. named it APJ in 19935. Comprising 380 amino acid residues, APJ features the characteristic 7-transmembrane domain structure, typical of a class A GPCR.
Nowadays, it is known that APLNR depicts physiological roles, including regulation of cardiovascular function, fluid homeostasis, the adipoinsular axis, gastrointestinal and immunomodulatory functions.
Apelin isoforms
Apelin (APLN) endogenous APJ ligand, is a 36-amino acids peptide, initially discovered in bovine stomach extracts. It is expressed and released by cultured adipocytes from a 77-amino acids prepropeptide, whose sequence was identified in human and bovine tissues, with the last 23 residues of the C terminus being identical in mammals.
Cleavage of this preproapelin at specific sites generates different isoforms, including apelin-36, apelin-17, apelin-13, and [Pyr1]apelin-13, which all act as agonists at the apelin receptor and equipotent mediators of vascular tone and cardiac contractility in human tissues in vitro. All of these predicted isoforms have been shown to be present in vivo, but the predominant isoforms in plasma are [Pyr1]apelin-13, apelin-13 and apelin-17, with [Pyr1]apelin-13 and apelin-13. Among these, [Pyr1]apelin-13 and apelin-13 are notably robust activators of apelin receptors in cell lines, while apelin-36 demonstrates remarkable efficacy as an inhibitor of HIV infection in vitro.
[Pyr1]apelin-13 peptide
Although apelin-36 is the most widely expressed APLN isoform, apelin-13 remains the more potent and abundant peptide in blood circulation. Notably, [Pyr1]apelin-13 (CAS: 217082-60-5) is the predominant isoform in human cardiac tissue, showcasing its physiological significance in regulating cardiovascular function.
SB-PEPTIDE is pleased to offer [Pyr1]apelin-13, as well as apelin-36 (see apelin-36 webpage), for further research into their multifaceted functions and therapeutic applications. |
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