Apilimod阿匹莫德,870087-36-8

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Apilimod mesylate

CAS No. : 870087-36-8

MCE 国际站：Apilimod mesylate

产品活性：Apilimod (STA 5326) mesylate 是 IL-12/IL-23 的有效抑制剂，抑制人和猴的 PBMC 细胞中的 IL-12，IC₅₀ 值为 1 nM 和 2 nM。Apilimod 是一种有效且高度选择性的 PIKfyve 抑制剂。

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

作用靶点：Interleukin Related  |  PIKfyve

In Vitro: Apilimod inhibits IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC₅₀ of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod.

In Vivo: Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. Apilimod causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis.

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