| Description | ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2. |
| In vitro | ACH-000143在MT1/MT2受体上展现了亚nM级的效能，同时在啮齿动物中具有高度的口服生物利用度，偏向外周的药物暴露率，以及在广泛目标群体中的优秀选择性。 |
| In vivo | 连续两月口服给予高脂饮食大鼠ACH-000143，其体重增长的减少效果与dapagliflozin相似，但在改善肝脂肪变性和三酸甘油脂水平方面表现出更优异的结果。 |
| Target activity | MT1:0.06 nM(EC50), MT2:0.32 nM(EC50) |
| molecular weight | 297.74 |
| Molecular formula | C13H16ClN3O3 |
| CAS | 2225836-30-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/ml (201.52 mM) |
| References | 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. |