Apilimod mesylate

SKU: orb1223019

Description

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

Key Properties

• CAS Number: 870087-36-8
• MW: 610.7
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₄N₆O₈S₂
• SMILES: Cc1cccc(c1)/C=N/Nc1nc(nc(c1)N1CCOCC1)OCCc1ccccn1.CS(=O)(=O)O.CS(=O)(=O)O
• Target: AChR
• Solubility: In Vitro: H2O : 100 mg/mL (163.75 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

AChR