| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
T77012-5mg促销 |
98.80% | ￥208.00 ￥166.00 |
6 | - | - | - | - |
|
T77012-10mg促销 |
98.80% | ￥320.00 ￥256.00 |
6 | - | - | - | - |
|
T77012-25mg促销 |
98.80% | ￥670.00 ￥536.00 |
5 | - | - | - | - |
|
T77012-100mg |
≥98% | ￥1710.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM) | ||||||||||||||||||||
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| 靶点： | Dopamine Receptor;DopamineReceptor | ||||||||||||||||||||
| 体外研究： | 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. | ||||||||||||||||||||
| 参考文献： | 1. Free RB, et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol. 2014;86(1):96-105. 2. Chun LS, et al. Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor. Front Synaptic Neurosci. 2018;10:2. Published 2018 Feb 21. |
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| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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