ACH-000143 是一种可口服的褪黑素受体激动剂,对 MT1 和 MT2 的EC50值分别为0.06 和0.32 nM。
产品描述
ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.
体外活性
ACH-000143 demonstrated subnanomolar potency at MT1/MT2 receptors, high oral bioavailability in rodents, peripherally preferred exposure, and excellent selectivity in a broad panel of targets.
体内活性
Two-month oral administration of ACH-000143 in high-fat diet rats led to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels.
Cas No.
2225836-30-4
分子式
C13H16ClN3O3
分子量
297.74
储存和溶解度
DMSO:60 mg/ml (201.52 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years