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Apilimod

CAS No. : 541550-19-0

MCE 站：Apilimod

产品活性：Apilimod (STA 5326) 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. TA-5326 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Oxygen Sensing Compound Library  |  Anti-COVID-19 Compound Library  |  Glycolysis Compound Library  |  Pyroptosis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Resatorvid  |  Disulfiram  |  Tocilizumab  |  Diacerein  |  Vidofludimus  |  LMT-28  |  Muscone  |  SC144  |  Hydrocortisone hemisuccinate  |  RCGD423  |  Neochlorogenic acid  |  Y-320  |  Ginsenoside Rh1  |  Semapimod tetrahydrochloride  |  Pectolinarin  |  Ginsenoside Rc  |  Mulberroside A  |  Madecassic acid  |  Methylthiouracil  |  Balsalazide  |  Kaempferol 3-O-β-D-glucuronide  |  Reslizumab  |  Suplatast (Tosilate)  |  Vacuolin-1  |  YQ128  |  Ginsenoside F3  |  Tyrphostin A1  |  Dexanabinol  |  Eucalyptol

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