MS48107是一种有效的 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂。它对 GPR68 的选择性高于相关的质子 GPCR、神经递质转运蛋白和 hERG 离子通道,并能轻松穿越小鼠的血脑屏障 (BBB)。
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描述 | MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). It shows selectivity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can effectively cross the blood-brain barrier (BBB) in mice[1]. |
体内研究 | A single intraperitoneal injection of MS48107 at a dose of 25 mg/kg results in substantial exposure levels (exceeding 10 μM) in both plasma and brain within 0.5 hours in Swiss Albino mice. These elevated levels persist in both plasma and brain for a duration of 2 hours [1]. |
体外研究 | 5-HT2B exhibits moderate binding affinity for MS48107, characterized by a Ki value of 219 nM. While MS48107 demonstrates no agonist activity at 5-HT2B receptors, it manifests weak antagonist activity with a Ki value of 310 nM[1]. MS48107 exhibits agonist activity exclusively at the MT1 and MT2 receptors. Specifically, it functions as a weak full agonist at the MT1 receptor (EC50 = 320 nM) and as a weak partial agonist at the MT2 receptor (EC50 = 540 nM). Furthermore, MS48107 demonstrates low binding affinities for both MT1 (5900 nM) and MT2 (1100 nM) receptors [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
11.98mL 2.40mL 1.20mL |
23.96mL 4.79mL 2.40mL |
CAS号 | 2375070-79-2 |
分子式 | C23H20FN5O2 |
分子量 | 417.436 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(251.54 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |