In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 and IL-12p40 production, with IC50s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 with an IC50 of 5.2 nM. APY0201 demonstrates ameliorated inflammation in an experimental model of colitis.
In vivo: Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment.
|Cell lines||Mouse TG-PEC or human PBMC|
|Preparation method||Mouse TG-PEC or human PBMC are incubated with APY0201 (1, 10, 100, 1000 and 10000 nM) in the presence of 100 ng/mL mouse or human IFN-γ and 0.05%w/v Staphylococcus aureus Cowan I strain (SAC).|
|Concentrations||1, 10, 100, 1000 and 10000 nM|
|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.
|Solubility||DMSO: ≥ 30 mg/mL|
Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201.
Hayakawa N, et al. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9. PMID: 24767819.
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