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Apremilast
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Apremilast图片
CAS NO:608141-41-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
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; Apremilast; CC 10004; Otezla (Trade name)
SMILES Code CC(NC1=CC=CC(C(N2[C@@H](C3=CC=C(OC)C(OCC)=C3)CS(=O)(C)=O)=O)=C1C2=O)=O
实验参考方法
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 Arthritis Res Ther. 2015 Sep 15;17:249; J Chromatogr Sci. 2016 Sep;54(8):1336-40.