AQX-016A 是一种口服有效的SHIP1激动剂。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。
| 生物活性 | AQX-016A is an orally active and potentSHIP1agonist. AQX-016A can activate recombinantSHIP1enzymein vitroand stimulateSHIP1activity. AQX-016A also can inhibit thePI3Kpathway and TNFa production, can be useful for various inflammatory diseases research[1][2]. |
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体外研究
(In Vitro) | AQX-016A (5 μg/mL, 30 min) inhibits the PI3K-mediated increase in intracellular PIP3 levels, and reduces PIP3 levels through 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, p38MAPKand extracellular signal-regulated kinase (ERK) in SHIP1+/+but not in SHIP1-/-mast cells. |
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体内研究
(In Vivo) | AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia[1][2].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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