MLS-1547 是一种高效的 G 蛋白偏向多巴胺 D2 受体 (D2R) 激动剂 (Ki\u003d1.2 μM)。
货号:ajcx19822
CAS:315698-36-3
分子式:C19H19ClN4O
分子量：354.8
溶解度:DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MLS-1547 is a G protein-biased agonist of dopamine D2 receptors (EC50 = 0.37 μM in a calcium mobilization assay).1 It inhibits forskolin-induced cAMP accumulation in CHO cells expressing human D2 receptors (EC50 = 0.26 μM) but is inactive in β-arrestin recruitment assays. MLS-1547 antagonizes dopamine-induced β-arrestin recruitment in cell-based assays with IC50 values ranging from 3.8 to 9.9 μM.1 It is also an inhibitor of type II secretion in Gram-negative bacteria.2 MLS-1547 inhibits secretion of phospholipase C (PlcH/N) and the virulence factor elastase (LasB) from P. aeruginosa (IC50s = 15 and 13 μM, respectively) and inhibits B. pseudomallei protease secretion by 90.8% when used at a concentration of 25 μM.

|1. Free, R.B., Chun, L.S., Moritz, A.E., et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol. Pharmacol. 86(1), 96-105 (2014).|2. Moir, D.T., Di, M., Wong, E., et al. Development and application of a cellular, gain-of-signal, bioluminescent reporter screen for inhibitors of type II secretion in Pseudomonas aeruginosa and Burkholderia pseudomallei. J. Biomol. Screen. 16(7), 694-705 (2011).