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Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂,可抑制实验性自身免疫性脑脊髓炎,有抗抑郁样活性。它优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。
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Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂,可抑制实验性自身免疫性脑脊髓炎,有抗抑郁样活性。它优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 628 | 现货 | |
5 mg | ¥ 1,570 | 现货 | |
10 mg | ¥ 2,570 | 现货 | |
25 mg | ¥ 4,230 | 现货 | |
50 mg | ¥ 5,900 | 现货 | |
100 mg | ¥ 8,120 | 现货 | |
500 mg | ¥ 16,200 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,930 | 现货 |
产品描述 | Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. |
靶点活性 | MT2 receptor:10.2 nM(ki), MT1 receptor:158 nM(ki) |
体外活性 | Luzindole (5-10 μg/ml) suppresses antigen-specific proliferation of the MBP-reactive LV-4 T cell line[1]. |
体内活性 | Luzindole (30 mg/kg i.p.) decreases the time of immobility in a dose-dependent manner, the effect being more pronounced at midnight (60% reduction) than at noon (39% reduction). Luzindole (30 mg/kg; i.p.; days 0-5) inhibits experimental autoimmune encephalomyelitis[2]. Luzindole (30 mg/kg i.p.) did not modify the time of immobility either at noon or midnight in the albino ND/4 mouse, or in the C57BL/6J mouse, which does not produce melatonin[3]. The effect of luzindole is time-dependent, showing a maximal effect at 60 min. The anti-immobility effect of luzindole (10 mg/kg i.p.) is prevented by the administration of melatonin (30 mg/kg i.p.). |
别名 | N-乙酰-2-苄基色胺, N-0774 |
分子量 | 292.37 |
分子式 | C19H20N2O |
CAS No. | 117946-91-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (342.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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