(Glp1)-Apelin-13 (trifluoroacetate salt)

The apelin gene encodes a pre-proprotein that is processed to generate bioactive peptides consisting of 36, 17, or 13 amino acids: apelin-36 (Item No. 13524), apelin-17, and apelin-13 (Item No. 13523), 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.1,2 (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).1 (Glp1)-Apelin-13 is the major apelin isoform in the plasma of healthy human subjects.3 It can have vasoconstrictor and antipyretic effects in vitro and in vivo.4,5,6WARNING This product is not for human or veterinary use.

[1] KAZUHIKO TATEMOTO . Isolation and Characterization of a Novel Endogenous Peptide Ligand for the Human APJ Receptor[J]. Biochemical and biophysical research communications, 1998, 251 2: Pages 471-476. DOI: 10.1006/bbrc.1998.9489
[2] DENNIS K. LEE. Characterization of Apelin, the Ligand for the APJ Receptor[J]. Journal of Neurochemistry, 2001, 74 1: 34-41. DOI: 10.1046/j.1471-4159.2000.0740034.x
[3] EUGENE Y. ZHEN  Jesus A G  Richard E Higgs. Pyroglutamyl apelin-13 identified as the major apelin isoform in human plasma[J]. Analytical biochemistry, 2013, 442 1: Pages 1-9. DOI: 10.1016/j.ab.2013.07.006
[4] SIDATH D KATUGAMPOLA. [125I]-(Pyr1)Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man[J]. British Journal of Pharmacology, 2009, 132 6: 1255-1260. DOI: 10.1038/sj.bjp.0703939
[5] SHUNTARO KAGIYAMA. Central and peripheral cardiovascular actions of apelin in conscious rats[J]. Regulatory Peptides, 2005, 125 1: Pages 55-59. DOI: 10.1016/j.regpep.2004.07.033
[6] THOMAS HATZELMANN . Antipyretic effect of central [Pyr1]apelin13 on LPS-induced fever in the rat[J]. Regulatory Peptides, 2013, 184: Pages 6-13. DOI: 10.1016/j.regpep.2013.03.018