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A-804598 是一个 CNS 渗透,竞争性和选择性的 P2X7受体拮抗剂,作用于小鼠、大鼠和人的 P2X7 受体,IC50s 分别是 9、10 和 11 nM。
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A-804598 是一个 CNS 渗透,竞争性和选择性的 P2X7受体拮抗剂,作用于小鼠、大鼠和人的 P2X7 受体,IC50s 分别是 9、10 和 11 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 235 | 现货 | |
2 mg | ¥ 319 | 现货 | |
5 mg | ¥ 455 | 现货 | |
10 mg | ¥ 689 | 现货 | |
25 mg | ¥ 1,380 | 现货 | |
50 mg | ¥ 2,280 | 现货 | |
100 mg | ¥ 3,580 | 现货 | |
500 mg | ¥ 7,780 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human). |
靶点活性 | P2X7R (human):11 nM, P2X7R (rat):10 nM, P2X7R (rat):9 nM |
体外活性 | A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1] |
体内活性 | According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2] |
别名 | A 804598 |
分子量 | 315.37 |
分子式 | C19H17N5 |
CAS No. | 1125758-85-1 |
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: 31.5 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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