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APY0201

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。

  • 货号:
    TK0420
  • 规格:
    2mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

CAS No.1232221-74-7
生物活性APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
分子式C23H23N7O
分子量413.48
储存条件Powder -20℃ 3 years
溶解性数据DMSO : ≥ 35 mg/mL (84.65 mM)
体内研究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.
体外研究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.
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