Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AQX-016A 是一种口服有效的 SHIP1激动剂。AQX-016A 是 Pelorol 的结构类似物,在相同摩尔浓度下,其效力是海洋天然产物 Pelorol 的 3 倍。AQX-016A 可以在体外激活重组 SHIP1酶并刺激 SHIP1活性。AQX-016A 还可抑制 PI3K 通路和 TNFa 的产生,可用于各种炎症疾病的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 14,900 | 6-8周 | ||
50 mg | ¥ 19,420 | 6-8周 | ||
100 mg | ¥ 24,625 | 6-8周 |
产品描述 | AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A is a structural analog of pelorol which is 3 times more potent than the marine natural product pelorol at the same molar concentration. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research [1] [2]. |
体外活性 | AQX-016A (5 μg/mL, 30 min) inhibits the PI3K-mediated increase in intracellular PIP3 levels, and reduces PIP3 levels by activation of a 5 'phosphatase enzyme [1]. AQX-01 6A (0-5 μg/mL, 30 min) inhibits LPS-induced PKB phosphorylation in a SHIP dependent manner [1]. AQX-016A (0-5 μg/mL, 2 h) significantly inhibits TNFa in both J774 and peritoneal macrophages at both 1 and 5 μg/mL [1]. AQX-016A (0-6 μg/mL, 30 min) requires SHIP to maximally inhibit TNFa production in BMDM, selectively inhibits TNF production from SHIP1 +/+ but not SHIP1 -/- macrophages [1]. AQX-016A (0-5 μg/mL, 0-90 min) inhibits TNFa translation [1]. AQX-016A (0-15 μM, 30 min) increases SHIP1 enzyme activity in vitro and in intact cells, inhibits macrophage and mast-cell activation [2]. AQX-016A (15 μM, 30 min) inhibits immune cell activation, and inhibits PI3K-dependent macrophage and mast-cell responses in a SHIP-dependent manner [2]. Western Blot Analysis Cell Line: SHIP1 +/+ and SHIP1 -/- mast cells [2] Concentration: 0, 3, 6, 15, 30 μM Incubation Time: 30 min Result: Inhibited PIP3-regulated intracellular signal transduction events in SHIP-expressing hematopoietic cells, but not in SHIP-deficient hematopoietic or nonhematopoietic cells. Preferentially inhibited, in a dose-dependent manner, LPS-stimulated PKB phosphorylation in SHIP1 +/+ but not in SHIP1 -/- macrophages, and inhibited the phosphorylation of PKB, p38 MAPK and extracellular signal-regulated kinase (ERK) in SHIP1 +/+ but not in SHIP1 -/- mast cells. |
体内活性 | AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels and inhibits inflammation in a mouse model of endotoxemia [1] [2]. |
分子量 | 328.49 |
分子式 | C22H32O2 |
CAS No. | 849669-54-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AQX-016A 849669-54-1 AQX016A AQX 016A Inhibitor inhibitor inhibit