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    InvivoChem Cat #: V1558
    CAS #: 1232221-74-7Purity ≥98%

    Description: APY0201 (APY-0201; APY 0201) is a novel, potent and selective PIKfyve inhibitor with potential anti-inflammatory activity. It inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/23 production. It is a unique small molecular IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an experimental model of colitis.

    References: 2014 Jun 1;22(11):3021-9.

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    Molecular Weight (MW) 413.48 
    Formula C23H23N7O
    CAS No. 1232221-74-7                 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:  ≥ 35 mg/mL
    Water: <1 mg/mL
    Ethanol: N/A
    Other info

    Chemical Name: (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine


    InChi Code: InChI=1S/C23H23N7O/c1-17-3-2-4-18(13-17)16-25-27-21-15-23(29-9-11-31-12-10-29)30-22(26-21)14-20(28-30)19-5-7-24-8-6-19/h2-8,13-16H,9-12H2,1H3,(H,26,27)/b25-16+

    SMILES Code: CC1=CC(/C=N/NC2=NC3=CC(C4=CC=NC=C4)=NN3C(N5CCOCC5)=C2)=CC=C1


    APY0201; APY-0201; APY 0201.

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    In Vitro

    In vitro activity: APY0201 inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity is maintained across species.APY0201 works differently from anti-IL-12/23 antibodies and acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). 

    Cell Assay: Mouse TG-PEC or human PBMC are incubated with APY0201 (1, 10, 100, 1000 and 104 nM) in the presence of 100 ng/mL mouse or human IFN-γ and 0.05% w/v  Staphylococcus aureus Cowan I strain (SAC).

    In VivoOral 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
    Animal model
    Formulation & Dosage30 mg/kg

     2014 Jun 1;22(11):3021-9.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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