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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  | In stock | |
| 2 mg | ¥ 319  | In stock | |
| 5 mg | ¥ 455  | In stock | |
| 10 mg | ¥ 689  | In stock | |
| 25 mg | ¥ 1,380  | In stock | |
| 50 mg | ¥ 2,280  | In stock | |
| 100 mg | ¥ 3,580  | In stock | |
| 500 mg | ¥ 7,780  | 待询 | |
| 1 mL x 10 mM (in DMSO) | ¥ 490  | In stock | 
A-804598 相关产品
| 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 |  P2X7 receptor (rat):10 nM, P2X7 receptor (human):11 nM, P2X7 receptor (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 | 
| Smiles | C[C@H](N(C(=N)NC#N)c1cccc2ncccc12)c1ccccc1 | 
| 密度 | 1.17 g/cm3 (Predicted) | 
| 颜色 | White | 
| 物理性状 | Solid | 
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 31.5 mg/mL (99.88 mM), Sonication is recommended.   | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.34 mM), Sonication is recommended.  请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
溶液配制表  | |||||||||||||||||||||||||||||||
DMSO 
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