NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)

NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)

• CAS Number: 2891469-80-8
• UNSPSC Description: NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) can activate Gαi1 (EC50=0.8 nM) and recruit β-arrestin2 (EC50=31 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) exhibits prolonged cardiac effects[1].
• Target Antigen: Apelin Receptor (APJ)
• Type: Reference compound
• Related Pathways: GPCR/G Protein
• Applications: Neuroscience-Neuromodulation
• Field of Research: Cardiovascular Disease
• Assay Protocol: https://www.medchemexpress.com/nh2-c-x-r-l-s-x-k-g-p-d-1nal.html
• Solubility: H2O
• Smiles: 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=C4C=CC=CC4=CC=C3)C(O)=O)=O)=O)=O)CCCCN)=O)C/C=C\C1)=O)CO)=O)CC(C)C)=O)CCCNC(N)=N)=O
• Molecular Weight: 1020.18
• References & Citations: [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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported