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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].
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].
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | 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. |
分子量 | 348.37 |
分子式 | C20H17FN4O |
CAS No. | 461449-78-5 |
存储 | Shipping with blue ice. |
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