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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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.
cGAMP is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA.
N6-isopentenyladenosine is a plant hormone.
X-α-Gal is suitable as a substrate for α-galactosidase.
RU320521 (also known as RU521; RU.521) is a potent and selective inhibitor of cGAS, inhibiting cGAS-mediated interferon upregulation.
|Dextran sulfate sodium salt
Dextran sulfate sodium salt is a polyanionic derivative of dextran produced by esterification of Dextran with chlorosulphonic acid.
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