中文名 | IQ-1S (free acid) |
英文名 | IQ-1S (free acid) |
别名 | 化合物IQ-1S 11H-茚并[1,2-B]喹喔啉-11-酮肟 11H-茚并[1,2-b]喹喔啉-11-酮肟 |
英文别名 | IQ1S IQ-1S IQ 1S IQ-1S CS-2230 IQ-1 sodium IQ-1S (free acid) 11H-Indeno[1,2-b]quinoxalin-11-one oxime Sodium |
CAS | 23146-22-7 |
化学式 | C15H9N3O |
分子量 | 247.25 |
溶解度 | DMSO: 溶解2mg/mL,澄清 (温热) |
存储条件 | Sealed in dry,2-8°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | Compound IQ-1S is a potent, noncytotoxic inhibitor of pro-inflammatory cytokine [interleukin (IL)-1α, IL-1β, IL-6, IL-10, tumor necrosis factor (TNF)-α, interferon-γ, and granulocyte-macrophage colony-stimulating factor] and nitric oxide production by human and murine monocyte/macrophages. The effect of IQ-1S is evaluated on LPS-induced cytokine production in human PBMCs. Among the 12 cytokines analyzed, LPS (200 ng/mL) consistently induces five (IL-1α, IL-1β, IL-6, IL-10, and TNF-α) in PBMCs compared with DMSO-treated control cells. Production of all of these cytokines is significantly inhibited by 20 μM IQ-1S. Among them, TNF-α production is inhibited completely by IQ-1 (>99%), the levels of IL-1α, IL-1β, and IL-10 are decreased by 85%, and IL-6 production is decreased by 33%. |
体内研究 | When mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1S) i.p., the serum exposure of the compound is also good, with AUC 0-12h values of 2.9 and 7.4 μM/h, respectively. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.044 ml | 20.222 ml | 40.445 ml |
5 mM | 0.809 ml | 4.044 ml | 8.089 ml |
10 mM | 0.404 ml | 2.022 ml | 4.044 ml |
5 mM | 0.081 ml | 0.404 ml | 0.809 ml |
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