Apilimod mesylate

Research use only, not for human use.

Apilimod mesylate is a potent IL-12/IL-23 inhibitor.

Apilimod mesylate is a potent IL-12/IL-23 inhibitor.

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.

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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Endocrinology/Hormones

AChR

IL-12| IL-23

Cancer|Inflammation/Immunology

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870087-36-8

610.7

C25H34N6O8S2

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (163.75 mM)

Cc1cccc(c1)/C=N/Nc1nc(nc(c1)N1CCOCC1)OCCc1ccccn1.CS(=O)(=O)O.CS(=O)(=O)O

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(-20℃)

With Ice Pack

≥ 2 years