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Apilimod mesylate

Cat. No. M9418
Apilimod mesylate Structure
Synonym:

STA 5326 mesylate

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 520 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Apilimod mesylate is a potent IL-12/IL-23 inhibitor, which inhibits the IL-12 production in cultures of IFN-γ/LPS–stimulated human PBMCs with an IC50 of 10 nM. Apilimod mesylate inhibited IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. In vivo, oral administration of either 5 mg/kg or 20 mg/kg Apilimod mesylate (STA-5326) reduced the severity of EAU on day 14 and 18. In addition, mice treated with 20 mg/kg STA-5326 showed significantly decreased severity of EAU by histopathological analysis.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 610.7
Formula C25H34N6O8S2
CAS Number 870087-36-8
Purity >98%
Solubility DMSO
Storage at -20°C
References

PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.
Cai X, et al. Chem Biol. 2013 Jul 25;20(7):912-21. PMID: 23890009.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Apilimod mesylate, STA 5326 mesylate supplier, inhibitors

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