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。

AQX-016A is an orally active and potent SHIP1 agonist. 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.

Solid

CD40 PI3K

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.
AQX-01 6A (0-5 μg/mL, 30 min) inhibits LPS-induced PKB phosphorylation in a SHIP dependent manner.
AQX-016A (0-5 μg/mL, 2 h) significantly inhibits TNFa in both J774 and peritoneal macrophages at both 1 and 5 μg/mL.
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.
AQX-016A (0-5 μg/mL, 0-90 min) inhibits TNFa translation.
AQX-016A (0-15 μM, 30 min) increases SHIP1 enzyme activity in vitro and in intact cells, inhibits macrophage and mast-cell activation.
AQX-016A (15 μM, 30 min) inhibits immune cell activation, and inhibits PI3K-dependent macrophage and mast-cell responses in a SHIP

AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. [1]Yau, Tien Yin. Novel strategies for antagonizing the phosphatidylinositol-3-kinase pathway in disease. University of British Columbia. 2010.
[2]. Ong CJ, et al. Small-molecule agonists of SHIP1 inhibit the phosphoinositide 3-kinase pathway in hematopoietic cells. Blood. 2007 Sep 15;110(6):1942-9.