ms48107

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

MS48107 是一种有效的选择性 G 蛋白偶联受体 68 (GPR68) 正变构调节剂。它对 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。它可以很容易地穿过小鼠的血脑屏障（BBB）。

MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). It is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It can readily cross the blood-brain barrier (BBB) in mice.

5-HT2B has moderate binding affinity to MS48107 (compound 71) with a Ki value of 219 nM. At 5-HT2B receptors, MS48107 shows no agonist activity but display weak antagonist activity with a Ki 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.

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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Others

Other Targets

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2375070-79-2

417.44

C23H20FN5O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (239.56 mM)

Nc1nc(-c(c(CO)ccc2)c2F)nc(NCc(cc2)ccc2Oc2ccccc2)n1

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(-20℃)

With Ice Pack

≥ 2 years