AQX-016A

Name: AQX-016A
Brand: TargetMol
SKU: T8996
Rating: 4.5 (1 reviews)

还可以

产品编号 T8996Cas号 849669-54-1

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。

AQX-016A

还可以

产品编号 T8996Cas号 849669-54-1

规格	价格	库存
25 mg	¥ 14,900	6-8周
50 mg	¥ 19,420	6-8周
100 mg	¥ 24,625	6-8周

大包装 & 定制

加入购物车

实验操作小课堂

联系我们获取更多批次信息

资源下载

产品操作手册

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性

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].