ACH-000143

ACH-000143 is a potent, orally active, and peripherally preferred melatonin receptor agonist. It demonstrates subnanomolar potency at the MT1 (EC50 = 0.06 nM) and MT2 (EC50 = 0.32 nM) melatonin receptors, with high oral bioavailability in rodents and excellent selectivity across a broad panel of targets[1][2][4]. In preclinical studies, ACH-000143 reduced liver triglycerides and hepatic steatosis in diet-induced obese rats, showing efficacy comparable to dapagliflozin for weight gain reduction but superior effects on hepatic endpoints[3][5]. The compound is structurally related to benzimidazole derivatives and was designed to preferentially act in peripheral tissues rather than the central nervous system. Early toxicological assessments indicated no hERG binding or genotoxicity at doses up to 100 mg/kg orally[3][5]. The drug was developed by Aché Laboratórios Farmacêuticos as a candidate for metabolic diseases such as obesity, diabetes, and nonalcoholic steatohepatitis[2].

Other names

10b