Apilimod

541550-19-0

C23H26N6O2

DMSO : >= 46 mg/mL (109.92 mM)

Immunology/Inflammation

Apilimod is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-gamma/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. IC50 & Target: IC50: 1 nM (IL-12, human PBMCs), 2 nM (IL-12, monkey PBMCs) In Vitro: Apilimod inhibited IFN-gamma production induced by either IFN-gamma/SAC or SAC in human PBMCs, with an IC₅₀ of approximately 20 nM. Apilimod show some inhibition against IFN-gamma/SAC-induced TNF-alpha and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1beta, 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-gamma/LPS or IFN-gamma/SAC, and are completely suppressed by 100 nM Apilimod^[1]. 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^[1]. 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^[2].