Apremilast

SKU: orb1304839

Description

Apremilast

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 608141-41-9
• MW: 460.50
• Purity: 98.13%
• Formula: C₂₂H₂₄N₂O₇S
• SMILES: [C@H](CS(C)(=O)=O)(N1C(=O)C=2C(C1=O)=CC=CC2NC(C)=O)C3=CC(OCC)=C(OC)C=C3
• Target: Apoptosis,PDE,TNF
• Solubility: DMSO:58.33 mg/mL (126.67 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.17 mM)

Bioactivity

• Target IC50:
  PDE4:74 nM
• In Vitro:
  Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM ( IC50 6.9 ± .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 wit 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.
• Cell Research:
  Apremilast is solubilized in DMSO and stored, and then diluted with appropriate media (DMSO 0.025%) before us. Raw 264. 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 a the indicated concentration . 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 li and 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 wit the Mouse TNF-α Quantikine ELISA Kit. IC50 (EC50) calculations are made using non-linear regression, sigmoidal dose-response, constrainin the top to 100 % and bottom to 0 %, allowing variable slope, using GraphPad Prism v6.0.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

lipopolysaccharide, inhibit, LPS, PDE4, PBMC, nucleotide, orally, Inhibitor, Apremilast, Apoptosis, available, CC 10004, CC10004, CC-10004, cyclic, phosphodiesterase, Phosphodiesterase (PDE), TNFR, TNF Receptor, type-4, Tumor Necrosis Factor Receptor

Compound Identifiers

PubChem CID

11561674