LIT01-196

LIT01-196 is a metabolically resistant synthetic analog of apelin-17, designed to act as a potent and selective agonist of the Apelin receptor (ApelinR/APLNR). Apelin is an endogenous neurovasoactive peptide that increases cardiac contractility, promotes diuresis, and reduces vascular resistance but has a very short in vivo half-life. LIT01-196 was developed to overcome this limitation by enhancing metabolic stability and prolonging its biological effects. Preclinical studies demonstrate that LIT01-196 improves left ventricular function, increases cardiac vascular density, reduces cardiac remodeling and fibrosis after myocardial infarction (MI), and does so without lowering arterial blood pressure. It also acts centrally to inhibit vasopressin release and peripherally at the kidney to increase aqueous diuresis by reducing water reabsorption—making it potentially useful for treating heart failure post-MI as well as conditions involving water retention or hyponatremia[1][5]. The drug has shown high affinity for the Apelin receptor (Ki = 0.08 nM) with significantly improved plasma stability compared to native peptides[5].

Other names

apelin-17 analogapelin17 analogapelin 17 analogmetabolically resistant apelin-17 analog