化合物 MRK-623 T61176

Product Introduction
Bioactivity


英文名: MRK-623

描述: MRK-623 (Compound 14k) is a potent, orally active agonist of the GABA A receptor, exhibiting high affinity for subunits α1, α2, α3, and α5 with Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM, respectively. Notably, MRK-623 demonstrates anxiolytic effects [1].

体外活性: MRK-623 shows efficacy at human GABAA receptor subtypes expressed in L(tk - ) cells measured by whole cell patch-clamp electrophysiology [1].

体内活性: MRK-623 (oral gavage; 0.3, 1, and 3 mg/kg; once) shows anxiolytic effects in the rat elevated plus maze assay [1]. Animal Model: Rat Dosage: 0.3, 1, and 3 mg/kg Administration: Oral gavage; 0.3, 1, and 3 mg/kg; once Result: Showed 78% BZ site occupancy at 3 mg/kg, with an ID 50 of 0.8 mg/kg.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途