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    Apremilast
    Apremilast

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0082
    CAS #: 608141-41-9 Purity ≥98%

    Description: Apremilast (also known as CC-10004), a thalidomide analog, is a novel and orally bioavailable small molecule inhibitor of the phosphodiesterase 4 (PDE4) with potential anti-inflammatory activity. It regulates inflammation through multiple cAMP downstream effectors. Apremilast inhibits PDE4 with an IC50 of 74 nM using 1 μM cAMP as substrate. Apremilast inhibits spontaneous production of TNF-alpha from human rheumatoid synovial cells. Apremilast was approved by the FDA in 2014 for treatment of adults with active psoriatic arthritis. It is also being tested for its efficacy in treating other chronic inflammatory diseases such as ankylosing spondylitis, Behcet's disease, and rheumatoid arthritis.

    References:  2015 Sep 15;17:249;

    Related CAS: 253168-86-4 [Apremilast, (+/-)-; Otezla]

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    Molecular Weight (MW) 460.50
    Formula C22H24N2O7S
    CAS No. 608141-41-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility(In vitro)DMSO: >90 mg/mL 
    Water: <1 mg/mL 
    Ethanol: 3 mg/mL 
    Chemical Name (S)-N-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide
    Synonyms CC-10004; CC10004; CC 10004; Otezla (Trade name)
    SMILES Code CC(NC1=CC=CC(C(N2[[email protected]@H](C3=CC=C(OC)C(OCC)=C3)CS(=O)(C)=O)=O)=C1C2=O)=O


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    In Vitro

    In vitro activity: Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM (pIC50=6.98±0.2), which almost exactly replicates previous reported TNF-α inhibition by Apremilast on peripheral blood mononuclear cells (PBMCs) (IC50=110 nM) and which is similar to the potency of Apremilast for PDE4 enzymatic inhibition (IC50=74 nM). These results are clearly consistent with the hypothesis that Apremilast inhibits TNF-α by increasing intracellular cAMP levels. PKA, Epac1 and Epac2 knockdowns prevented TNF-α inhibition and IL-10 stimulation by Apremilas. 


    Kinase Assay: Quantification of cytokines and chemokines was performed using Luminex x-MAP technology (Luminex Corp, Austen TX, USA). Tissue culture supernatants and mouse exudates were analyzed for expression of IL-1α, IL-6 and IL-10 using a Milliplex multi-analyte magnetic bead panel from EMD Millipore (MCYTOMAG-70K, Billerica, MA, USA). Assays were performed according to the kit protocol using the appropriate matrix solution (culture media or PBS for supernatants and exudates, respectively). Data were collected on a Luminex 200 instrument and analyzed using Analyst 5.1 software (Millipore) with four-parameter logistic curve fitting. Samples were assayed in duplicate. All standard curves generated from the known reference cytokine concentrations supplied by the manufacturer had R2 values calculated at or close to 1 and percent recovery between 80 and 120 %. Quality controls included with each kit performed as expected.


    Cell Assay: Raw 264.7 cells (100,000) are grown in 96-well plates. After 24 h, cells are stimulated with vehicle (final concentration of 0.025% DMSO) or with Apremilast at the indicated concentrations. After 30 minutes cells are stimulated with LPS 1 μg/mL for 4 h. When studying CGS21680 , SCH58261, ZM241385, BAY60-6583, or GS6201, the adenosine receptor ligands are added 15 minutes before Apremilast. Methotrexate is added 24 h and 1 h before Apremilast. Supernates are then collected and TNF-α levels are quantified with the Mouse TNF-α Quantikine ELISA Kit. IC50 (EC50) calculations are made using non-linear regression, sigmoidal dose-response, constraining the top to 100 % and bottom to 0 %, allowing variable slope, using GraphPad Prism v6.00.

    In VivoApremilast significantly reduces epidermal thickness and proliferation in vivo, it decreases the general histopatho-logical appearance of psoriasiform features and reduces expression of TNF-α, human leukocyte antigen-DR and intercellularadhesion molecule-1 in the lesioned skin.
    Animal model Mouse xenograft model of psoriasis (Beige-SCID mice)
    Formulation & Dosage Dissolved in 0.5% carboxymethylcellulose and 0.25% Tween 80; 5 mg/kg; P.O.
    References  2015 Sep 15;17:249;  2016 Sep;54(8):1336-40.


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

    Apremilast

    Apremilast and methotrexate (MTX) prevent inflammation in the air pouch independently.  2015 Sep 15;17:249.

     

    Apremilast

    Apremilast inhibits lipopolysaccharide (LPS)-induced TNF-α release via cyclic adenosine monophosphalphate (cAMP).  2015 Sep 15;17:249.

     

    Apremilast

    Effect of Protein kinase A (PKA), Exchange protein directly activated by cAMP (Epac)1 and Epac2 knockdown on the action of apremilast.  2015 Sep 15;17:249.


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