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Apremilast

SKU: orb1304839

Description

Apremilast (CC-10004) is an orally bioavailable, small-molecule PDE4 inhibitor exhibiting potent anti-inflammatory activity (IC50=74 nM). It is widely used in research to investigate inflammatory pathways, with applications in both in vitro cellular assays and in vivo models of autoimmune and inflammatory diseases.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Apremilast

Key Properties

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CAS Number608141-41-9
MW460.50
Purity99.95% (May vary between batches)
FormulaC22H24N2O7S
SMILES[C@H](CS(C)(=O)=O)(N1C(=O)C=2C(C1=O)=CC=CC2NC(C)=O)C3=CC(OCC)=C(OC)C=C3
TargetPDE,TNF,Apoptosis
SolubilityDMSO:58.33 mg/mL (126.67 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.17 mM)

Bioactivity

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Target IC50
PDE4:74 nM
In Vitro
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.
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Cell Research
Apremilast is solubilized in DMSO and stored, and then diluted with appropriate media (DMSO 0.025%) before use. 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.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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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

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
11561674 ↗

Key Properties

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No computed properties available.

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Apremilast (orb1304839)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 ml x 10 mM (in DMSO)
¥ 1,170.00
5 mg
¥ 1,170.00
10 mg
¥ 1,300.00
25 mg
¥ 1,560.00
100 mg
¥ 1,820.00
200 mg
¥ 2,600.00
500 mg
¥ 4,030.00
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