阿普司特 T2923

Product Introduction
Bioactivity


英文名: Apremilast

描述: Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 抑制剂，IC50为 74 nM。它抑制脂多糖释放TNF-α，IC50为 104 nM。

细胞实验: Apremilast is solubilized in DMSO and stored, and then diluted with appropriate media (DMSO 0.025%) before use[1]. 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[1].

体外活性: 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 Apremilast[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.6 mg/mL (10 mM)


关键字: TNFR | orally | TNF Receptor | nucleotide | inhibit | lipopolysaccharide | LPS | Apoptosis | phosphodiesterase | CC 10004 | PBMC | Tumor Necrosis Factor Receptor | CC10004 | Apremilast | cyclic | Phosphodiesterase (PDE) | available | Inhibitor | type-4

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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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