APJ receptor agonist 4

APJ receptor agonist 4 is a potent and oral active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

apelin receptor[1]

Assessment of Pharmacokinetics (PK) profile of APJ receptor agonist 4 (compound 21) in mouse[1]. species rat monkey dogmax (ng/mL) dose (mg/kg) 1 (i.v. and p.o.) 1 (i.v.) and 3 (p.o.) 1 (i.v. and p.o.) vehiclea F G G CI (mL/min/kg) 4.6 10.6 2.4 VSS (L/kg) 1.6 0.2 0.2 T1/2 (h) 4.0 1.3 2.5 Cmax (μM•h) 2.2 1.4 6.5 AUC0-24 (μM•h) 3.7 2.5 14.2 F (%) 54 27 76 a: Vehicle F: 5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9 and vehicle G: 10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9.

[1]. Meng W, et al. Identification of a Hydroxypyrimidinone Compound (21) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure. J Med Chem. 2021;64(24):18102-18113.