Description

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life[1].—Neuroscience-Neuromodulation–C49H73N13O11—-[1]Tran K, et, al. Size-Reduced Macrocyclic Analogues of [Pyr 1]-apelin-13 Showing Negative Gα 12 Bias Still Produce Prolonged Cardiac Effects. J Med Chem. 2022 Jan 13;65(1):531-551. –2891469-81-9–1020.18—-N[C@@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N2CCC[C@H]2C(N[C@H](CC3=CC=C4C=CC=CC4=C3)C(O)=O)=O)=O)=O)CCCCN)=O)C/C=CC1)=O)CO)=O)CC(C)C)=O)CCCNC(N)=N)=O–Cardiovascular Disease–10 mM in DMSO–Apelin Receptor (APJ)—-GPCR/G Protein–Peptides