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APY0201

CAS No. : 1232221-74-7

MCE 站：APY0201

产品活性：APY0201 是一种有效的 PIKfyve 抑制剂，抑制 PtdIns3P 转化为PtdIns(3,5)P₂，IC₅₀ 为 5.2 nM。 APY0201 还抑制 IL-12/IL-23 产生。

研究领域：PI3K/Akt/mTOR  |  Immunology/Inflammation

作用靶点：PIKfyve  |  Interleukin Related

In Vitro: APY0201 works differently from anti-IL-12/23 antibodies ａnd acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 ａnd IL-12p40 production, with IC₅₀s of 8.4 ａnd 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 ａnd IL-12p40 over TNF-α, ａnd this selectivity is maintained across species.

In Vivo: Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment.

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