MLS1547 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂,Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导,EC50 为 0.37 μM。
产品描述
MLS1547 is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assay.
体外活性
MLS1547 fully antagonizes dopamine-mediated β-arrestin recruitment to the D2 dopamine receptor with an IC50 of 9.9 μM in the DiscoveRx assay and 3.8 μM in the BRET assay. MLS1547 is found to completely displace [3H]methylspiperone binding to the D2 dopamine receptor, with a calculated Ki of 1.2 μM[2].
Cas No.
315698-36-3
分子式
C19H19ClN4O
分子量
354.83
别名
MLS 1547;MLS000051547;MLS-1547
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years