MS48107,2375070-79-2

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MS48107

CAS No. : 2375070-79-2

MCE 国际站：MS48107

产品活性：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。MS48107 对 GPR68 的选择性高于密切相关的质子 GPCR，神经递质转运蛋白和 hERG 离子通道。MS48107 可以轻松穿越小鼠的血脑屏障 (BBB)。

研究领域：GPCR/G Protein

作用靶点：GPR68

In Vitro: 5-HT2B has moderate binding affinity to MS48107 (compound 71) with a K_i value of 219 nM. At 5-HT2B receptors, MS48107 shows no agonist activity but display weak antagonist activity with a K_i value of 310 nM, respectively.
MS48107 (compound 71) has agonist activity only at the MT1 and MT2 receptors. MS48107 is a weak full agonist at the MT1 receptor (EC₅₀ = 320 nM) and a weak partial agonist activity at the MT2 receptor (EC₅₀ = 540 nM). MS48107 displays low binding affinities to MT1 (5900 nM) and MT2 (1100 nM) receptors.

In Vivo: For MS48107 (compound 71), a single intraperitoneal injection at the dose of 25 mg/kg leads to high exposure levels (above 10 μM) in both plasma and brain at 0.5 h in mice (Swiss Albino mice). The high compound exposure levels in both plasma and brain are maintained for 2 h.

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