型号:
产品价格:电议      采购度:1606      原产地:美洲
发布时间:2021/11/26 14:44:22 所属地区:国外 国外
简要描述:
APY0201 是一种有效的 PIKfyve 抑制剂,抑制 PtdIns3P 转化为PtdIns(3,5)P2,IC50 为 nM。 APY0201 还抑制 IL-12/IL-23 产生。
标签:apy-0201
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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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更新时间:2024/1/2 10:19:26
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