Uses
The apelin gene encodes a pre-proprotein that is processed to generate bioactive peptides consisting of 36, 17, or 13 amino acids: apelin-36 , apelin-17, and apelin-13 , respectively. Apelin-13 is an endogenous ligand of the APJ receptor, activating this G protein-coupled receptor with an EC50 value of 0.37 nM. (Glp1)-Apelin-13 is a pyroglutamylated form of apelin-13, in that the N-terminal glutamine residue is cyclized to pyroglutamic acid. Like apelin-13, this compound is a potent APJ receptor agonist (EC50 = 0.30 nM). (Glp1)-Apelin-13 is the major apelin isoform in the plasma of healthy human subjects. It can have vasoconstrictor and antipyretic effects in vitro and in vivo.
Definition
ChEBI: P-Glu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe is a thirteen-membered polypeptide consisting of p-Glu, Arg, Pro, Arg, Leu, Ser, His, Lys, Gly, Pro, Met, Pro and Phe residues joined in sequence. It has a role as an apoptosis inhibitor, a neuroprotective agent and a human metabolite. It is a tautomer of a [Pyr1]apelin-13(2+).
Biological Activity
(Pyr1)-Apelin-13, the major apelin form in human plasma and heart, corresponds to Apelin-13 with posttranslationally modified pyroglutamyl (pGlu, pE) at the N-terminus instead of glutamine (Gln, Q). (Pyr1)-Apelin-13 exhibits higher APJ agonist potency than Apelin-13 (EC50 = 0.30 vs. 0.37 nM, respectively; acidification induction in human APJ-expresing CHO cell cultures). (Pyr1)-Apelin-13 is reactive toward human, murine, rat, and bovine species, and widely used for studyinhg APJ-mediated cellular and physiological functions both in cultures and in animals in vivo (via intraperitoneal, intravenous, intrathecal injection).
in vivo
[Pyr1]-apelin-13 nanocarriers in a mouse model of pressure-overload induced heart failure demonstrate a sustainable long-term effect of [Pyr1]-apelin-13 in preventing cardiac dysfunction[1]. [Pyr1] apelin-13 (1, 5 μg) improves locomotor activity and reduces pain symptoms, cavity size and caspase-3 levels in rats. [Pyr1] apelin-13 (1, 5 μg) significantly increases thermal paw withdrawal latency. [Pyr1] apelin-13 in 5 μg dose also produces significant attenuation in paw withdrawal threshold compared to SCI animals from the second week post SCI[2].
