2. Metabolic Enzyme/Protease
    Apoptosis
  3. Phosphodiesterase (PDE)
    Apoptosis
    TNF Receptor
  4. Apremilast

Apremilast  (Synonyms: CC-10004)

Cat. No.: HY-12085 Purity: 99.87%
COA Handling Instructions

Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.

For research use only. We do not sell to patients.

Apremilast Chemical Structure

Apremilast Chemical Structure

CAS No. : 608141-41-9

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
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ready for reconstitution
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10 mg USD 77 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

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Description

Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].

IC50 & Target[1]

PDE4

74 nM (IC50)

In Vitro

Apremilast (CC-10004) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Apremilast (CC-10004), orally administered (5 mg/kg), significantly inhibits TNF-α production in the air pouch by 39 % (61±6 % of vehicle, P <0.001) and diminishes (by 28 %) the number of leukocytes present (72±12 % of vehicle, P<0.05). In agreement, immunohistologic analysis shows that neutrophil accumulation in the air pouch membrane is dramatically reduced by Apremilast. In the murine air pouch model, both Apremilast and methotrexate (MTX) significantly inhibit leukocyte infiltration, while Apremilast, but not MTX, significantly inhibits TNF-α release. The addition of MTX (1 mg/kg) to Apremilast (5 mg/kg) yields no more inhibition of leukocyte infiltration or TNF-α release than with Apremilast alone[1].
Apremilast is a novel, oral PDE4 inhibitor that has been shown to regulate inflammatory mediators. After oral administration of Apremilast, a mean maximum plasma concentration (Cmax) is found to be 67.00±14.87 ng/mL. The plasma concentration of Apremilast decreases rapidly and is eliminated from plasma with a terminal half-life of 0.92±0.46 h[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

460.50

Appearance

Solid

Formula

C22H24N2O7S
CAS No.
SMILES

CC(NC1=CC=CC(C(N2[[email protected]@H](C3=CC=C(OC)C(OCC)=C3)CS(=O)(C)=O)=O)=C1C2=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 44 mg/mL (95.55 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1716 mL 10.8578 mL 21.7155 mL
5 mM 0.4343 mL 2.1716 mL 4.3431 mL
10 mM 0.2172 mL 1.0858 mL 2.1716 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% CMC-Na  0.5% Tween-80

    Solubility: 5 mg/mL (10.86 mM); Suspened solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.43 mM); Suspended solution; Need ultrasonic

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.87%

COA (255 KB) RP-HPLC (189 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Mice[1]
Male mice are given weekly intraperitoneal injections of either MTX (1 mg/kg) or vehicle (PBS) for 4 weeks. Air pouches are generated by subcutaneous injection of 3 mL of sterile air and reinflated with 1.5 mL of sterile air 2 days later. Vehicle (0.5 % carboxymethylcellulose and 0.25 % Tween 80) or Apremilast (5 mg/kg) are orally dosed, with a syringe through a blunt-ended curved feeding tube, 24 h and 1 h before inflammation is induced on day 6 by injection of 1 mL of 2 % carrageenan suspension. Four hours later, mice are killed by CO2 narcosis, and exudates harvested with 2 mL PBS. Leukocytes are counted in a hemocytometer chamber and concentrations of cytokines are measured by ELISA or by the Luminex platform.
Rats[2]
Male Sprague Dawley rats (180-220 g) are used to study the pharmacokinetics of Apremilast. Diet is prohibited for 12 h before the experiment, but water is freely available. Blood samples (0.3 mL) are collected from the tail vein into heparinized 1.5 mL polythene tubes at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8 and 12 h after oral administration of Apremilast (6.0 mg/kg). The samples are immediately centrifuged at 4,000 g for 8 min. The plasma obtained (100 µL) is stored at −20°C until analysis. Plasma Apremilast concentration versus time data for each rat is analyzed by DAS (Drug and statistics) software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Apremilast608141-41-9CC-10004CC10004CC 10004Phosphodiesterase (PDE)ApoptosisTNF ReceptorTumor Necrosis Factor ReceptorTNFRorallyavailabletype-4cyclicnucleotidephosphodiesterasePDE-4,TNF-αlipopolysaccharideLPSPBMCInhibitorinhibitorinhibit

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