目錄:MedChemExpress LLC>>生化試劑>> MS48107 | MCE
CAS | 2375070-79-2 | 純度 | 99.75% |
---|---|---|---|
分子量 | 417.44 | 分子式 | C??H??FN?O? |
供貨周期 | 現貨 | 規格 | 5 mg |
貨號 | HY-134494 | 應用領域 | 醫療衛生,化工,生物產業,制藥 |
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CAS No. : 2375070-79-2
產品活性:MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
研究領域:GPCR/G Protein
作用靶點:GPR68
In Vitro: 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.
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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