2225836-30-4

ACH-000143 is a potent and orally active melatonin receptor agonist, with EC50 values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively[1].

ACH-000143 is a potent and orally active melatonin receptor agonist, with EC50 values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively[1]. ACH-000143 reduces liver triglycerides and steatosis in diet-Induced obese rats[1].ACH-000143 is devoid of hERG binding, genotoxicity, and behavioral alterations at doses up to 100 mg/kg p.o., supporting further investigation of this compound as a drug candidate[1].ACH-000143 significantly reduces plasma glucose at 10 mg/kg (-16.4%, p < 0.05) and 30 mg/kg (-16.9%, p < 0.01)[1].

MT1: 0.06 nM (EC₅₀); MT2: 0.32 nM (EC₅₀)

[1]. Marcos Antonio Ferreira Jr, et al. Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats. J Med Chem. 2021 Feb 25;64(4):1904-1929.