Apelin-36(human)

Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].

O=C(N[C@@H](C(C)C)C(N[C@@H](CCC(N)=O)C(N1[C@@H](CCC1)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(N)=O)C(NCC(N2[C@@H](CCC2)C(NCC(N3[C@@H](CCC3)C(N[C@@H](CC4=CNC5=CC=CC=C45)C(N[C@@H](CCC(N)=O)C(NCC(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CC6=CC=CC=C6)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N7[C@@H](CCC7)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CC8=CNC=N8)C(N[C@@H](CCCCN)C(NCC(N9[C@@H](CCC9)C(N[C@@H](CCSC)C(N%10[C@@H](CCC%10)C(N[C@@H](CC%11=CC=CC=C%11)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC(C)C)N

[1]Tatemoto K, Hosoya M, Habata Y, et al. Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor. Biochem Biophys Res Commun. 1998;251(2):471-476.|[2]Medhurst AD, Jennings CA, Robbins MJ, et al. Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin. J Neurochem. 2003;84(5):1162-1172.|[3]Zou MX, Liu HY, Haraguchi Y, Soda Y, Tatemoto K, Hoshino H. Apelin peptides block the entry of human immunodeficiency virus (HIV). FEBS Lett. 2000;473(1):15-18.|[4]Galon-Tilleman H, Yang H, Bednarek MA, et al. Apelin-36 Modulates Blood Glucose and Body Weight Independently of Canonical APJ Receptor Signaling. J Biol Chem. 2017;292(5):1925-1933.