MLS1547

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 在钙动员测定中刺激 D2R G 蛋白介导的信号传导，EC50 为 0.37 μM。

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.(In Vitro):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.

MLS1547 fully antagonizes dopamine-mediated β-arrestin recruitment to the D2R in the DiscoveRx assay, with an IC50 of 9.9 μM. Similar results were obtained when MLS1547 was examined for antagonist activity in the D2R β-arrestin BRET assay, demonstrating an IC50 of 3.8 μM. MLS1547 is found to completely displace [3H]methylspiperone binding to the D2R, with a calculated Ki of 1.2 μM.

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MLS-1547 | MLS 1547 | MLS000051547

GPCR/G Protein

Dopamine Receptor

SOD1

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315698-36-3

354.84

C19H19ClN4O

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (93.93 mM)

Oc1c(CN2CCN(CC2)c2ccccn2)cc(Cl)c2cccnc12

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(-20℃)

With Ice Pack

≥ 2 years