GLP-1 receptoragonist 3 is a GLP-1 receptoragonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.
GLP-1 receptoragonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of 64.5 nM, and is utilized in diabetes treatment research.
Thrombin receptoragonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .
APJ ReceptorAgonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.