1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

Apremilast (Synonyms: CC-10004)

Cat. No.: HY-12085 Purity: 99.87%
Data Sheet SDS Handling Instructions

Apremilast is a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Apremilast inhibits PDE4 with an IC50 of 74 nM using 1 μM cAMP as substrate.

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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Description

Apremilast is a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Apremilast inhibits PDE4 with an IC50 of 74 nM using 1 μM cAMP as substrate.

IC50 & Target

IC50: 74 nM (PDE4)[1]

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[1].

In Vivo

Apremilast, 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]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01634191 Celgene Corporation Healthy Volunteer February 2012 Phase 1
NCT01634178 Celgene Corporation|Celgene Healthy Volunteer February 2012 Phase 1
NCT02576678 Celgene Psoriasis October 13, 2015 Phase 2
NCT00521339 Celgene Corporation Psoriasis-Type Psoriasis|Plaque-Type Psoriasis August 2007 Phase 2
NCT01925768 Celgene Psoriatic Arthritis September 4, 2013 Phase 3
NCT01561963 Celgene Corporation Healthy February 2012 Phase 1
NCT03191539 Hospital Universitari Vall d'Hebron Research Institute|Celgene Corporation Arthritis; Psoriasis (Etiology) August 14, 2017 Phase 3
NCT03097003 Celgene Psoriasis April 6, 2017
NCT03096990 Celgene Arthritis, Psoriatic April 21, 2017
NCT00931242 Tufts Medical Center|Celgene Corporation Atopic Dermatitis|Allergic Contact Dermatitis June 2009 Phase 2
NCT03082729 University of Pennsylvania|Celgene Corporation|National Heart, Lung, and Blood Institute (NHLBI) Psoriasis|Cardiovascular Diseases April 24, 2017 Phase 4
NCT01200264 Duke University Chronic Plaque Psoriasis September 2010 Phase 2
NCT01250548 Baylor Research Institute Rheumatoid Arthritis May 2010 Phase 2
NCT02775500 University of California, San Diego|Celgene|The Organization of Teratology Information Specialists Psoriatic Arthritis|Psoriasis November 2014
NCT02425826 Celgene Parapsoriasis April 20, 2015 Phase 4
NCT01074502 University of North Carolina, Chapel Hill|Celgene Acne February 2010 Phase 2
NCT02236988 Celgene Corporation Healthy Volunteers January 2014 Phase 1
NCT02400749 Innovaderm Research Inc.|Celgene Palmo-plantar Psoriasis May 2015 Phase 4
NCT03000309 Derm Research, PLLC|Celgene Plaque Psoriasis December 29, 2016 Phase 4
NCT02307513 Celgene Behcet Syndrome December 16, 2014 Phase 3
NCT02641353 Celgene Corporation Healthy Volunteers January 2016 Phase 1
NCT01212770 Celgene Psoriatic Arthritis September 30, 2010 Phase 3
NCT01232283 Celgene Plaque Psoriasis November 2010 Phase 3
NCT01307423 Celgene Psoriatic Arthritis December 9, 2010 Phase 3
NCT01140503 Stanford University Dermatomyositis February 2010
NCT03123471 Celgene Psoriasis June 12, 2017 Phase 3
NCT01690299 Celgene Psoriasis|Psoriatic Arthritis October 1, 2012 Phase 3
NCT00866359 Celgene Corporation Behcet Syndrome October 2009 Phase 2
NCT01041625 Virginia Clinical Research, Inc.|Celgene Corporation Lichen Planus February 2010 Phase 2
NCT02558361 University of South Florida Psoriatic Arthritis April 2016 Phase 4
NCT02289417 Celgene Ulcerative Colitis December 10, 2014 Phase 2
NCT01583374 Celgene Ankylosing Spondyloarthritis May 2, 2012 Phase 3
NCT00944658 Imperial College London|Celgene Corporation Ankylosing Spondylitis August 2009 Phase 2
NCT02695212 Florida Academic Dermatology Centers Hidradenitis Suppurativa July 2016 Phase 2
NCT01285310 Celgene Corporation|Celgene Rheumatoid Arthritis December 2010 Phase 2
NCT01988103 Celgene Corporation Psoriasis;|Psoriatic Arthritis;|Psoriasis Arthropatica July 2013 Phase 2
NCT03160248 Technische Universität München|Celgene Corporation Nummular Eczema|Eczema|Dermatitis Eczema|Nummular Dermatitis June 2017 Phase 2
NCT00889421 Oregon Health and Science University|Celgene Corporation Uveitis November 2009 Phase 1|Phase 2
NCT01172938 Celgene Psoriatic Arthritis June 2010 Phase 3
NCT01212757 Celgene Psoriatic Arthritis September 27, 2010 Phase 3
NCT03049267 M.B.A. van Doorn|Celgene|Erasmus Medical Center Hidradenitis Suppurativa February 2, 2017 Phase 2
NCT01194219 Celgene Plaque Psoriasis September 2010 Phase 3
NCT02684123 Icahn School of Medicine at Mount Sinai Alopecia Areata February 2016
NCT00997581 Dartmouth-Hitchcock Medical Center|Celgene Corporation Acute Gout April 2010 Phase 2
NCT02412644 Psoriasis Treatment Center of Central New Jersey|Celgene Plaque Psoriasis April 2015 Phase 4
NCT02777554 Celgene Healthy Volunteers August 17, 2016 Phase 1
NCT02087943 Celgene Dermatitis, Atopic Dermatitis June 2014 Phase 2
NCT01045551 Julian M. Mackay-Wiggan|Celgene Corporation|Columbia University Erythematotelangiectatic Rosacea|Papulopustular Rosacea June 2010 Phase 2
NCT01200472 University of Erlangen-Nürnberg Medical School|Celgene Corporation Erosive Osteoarthritis of the Hand August 2010 Phase 2
NCT01204138 Stanford University|Celgene Corporation Arthritis, Rheumatoid September 2010 Phase 2
NCT03036995 Centre Hospitalier Universitaire de Nice Vitiligo March 20, 2017 Phase 2
NCT01393158 Oregon Health and Science University|Celgene Corporation Atopic Dermatitis
NCT02802735 Celgene Corporation Pharmacokinetics June 2016 Phase 1
NCT03175549 The Scripps Research Institute|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Alcohol Use Disorder July 2017 Phase 2
NCT03146247 Diamant Thaci|University of Luebeck Moderate to Severe Plaque Psoriasis June 15, 2017 Phase 4
NCT03123016 Icahn School of Medicine at Mount Sinai|Celgene Vitiligo April 14, 2017 Phase 2
NCT02954081 Prof. Kristian Reich|Sciderm GmbH Psoriasis January 2017
NCT00773734 Celgene Corporation Psoriasis|Plaque-type Psoriasis September 2008 Phase 2
NCT03022617 University of Alabama at Birmingham|Celgene Psoriatic Nail|Psoriasis Vulgaris|Psoriasis January 2017 Phase 4
NCT03168256 Can-Fite BioPharma Plaque Psoriasis February 2018 Phase 3
NCT02963779 Eli Lilly and Company Healthy December 2016 Phase 1
NCT00606450 Celgene Corporation|Celgene Psoriasis April 2006 Phase 2
NCT00701311 Kenneth Peters, MD|Celgene Corporation|William Beaumont Hospitals Prostatitis|Chronic Prostatitis With Chronic Pelvic Pain Syndrome June 2008 Phase 2
NCT00814632 Kenneth Peters, MD|Celgene Corporation|William Beaumont Hospitals Vulvodynia December 2008 Phase 2
NCT00456092 Celgene Corporation|Celgene Psoriatic Arthritis January 2009 Phase 2
NCT00869089 University Hospitals Cleveland Medical Center|Celgene Corporation Prurigo Nodularis September 2008 Phase 2
NCT00708916 New York University School of Medicine|Celgene Corporation Discoid Lupus Erythematosus June 2008 Phase 1|Phase 2
NCT00604682 Celgene Corporation Psoriasis January 2005 Phase 2
NCT01634191 Celgene Corporation Healthy Volunteer February 2012 Phase 1
NCT01634178 Celgene Corporation|Celgene Healthy Volunteer February 2012 Phase 1
NCT02576678 Celgene Psoriasis October 13, 2015 Phase 2
NCT00521339 Celgene Corporation Psoriasis-Type Psoriasis|Plaque-Type Psoriasis August 2007 Phase 2
NCT01925768 Celgene Psoriatic Arthritis September 4, 2013 Phase 3
NCT01561963 Celgene Corporation Healthy February 2012 Phase 1
NCT03191539 Hospital Universitari Vall d'Hebron Research Institute|Celgene Corporation Arthritis; Psoriasis (Etiology) August 14, 2017 Phase 3
NCT03097003 Celgene Psoriasis April 6, 2017
NCT03096990 Celgene Arthritis, Psoriatic April 21, 2017
NCT00931242 Tufts Medical Center|Celgene Corporation Atopic Dermatitis|Allergic Contact Dermatitis June 2009 Phase 2
NCT03082729 University of Pennsylvania|Celgene Corporation|National Heart, Lung, and Blood Institute (NHLBI) Psoriasis|Cardiovascular Diseases April 24, 2017 Phase 4
NCT01200264 Duke University Chronic Plaque Psoriasis September 2010 Phase 2
NCT01250548 Baylor Research Institute Rheumatoid Arthritis May 2010 Phase 2
NCT02775500 University of California, San Diego|Celgene|The Organization of Teratology Information Specialists Psoriatic Arthritis|Psoriasis November 2014
NCT02425826 Celgene Parapsoriasis April 20, 2015 Phase 4
NCT01074502 University of North Carolina, Chapel Hill|Celgene Acne February 2010 Phase 2
NCT02236988 Celgene Corporation Healthy Volunteers January 2014 Phase 1
NCT02400749 Innovaderm Research Inc.|Celgene Palmo-plantar Psoriasis May 2015 Phase 4
NCT03000309 Derm Research, PLLC|Celgene Plaque Psoriasis December 29, 2016 Phase 4
NCT02307513 Celgene Behcet Syndrome December 16, 2014 Phase 3
NCT02641353 Celgene Corporation Healthy Volunteers January 2016 Phase 1
NCT01212770 Celgene Psoriatic Arthritis September 30, 2010 Phase 3
NCT01232283 Celgene Plaque Psoriasis November 2010 Phase 3
NCT01307423 Celgene Psoriatic Arthritis December 9, 2010 Phase 3
NCT01140503 Stanford University Dermatomyositis February 2010
NCT03123471 Celgene Psoriasis June 12, 2017 Phase 3
NCT01690299 Celgene Psoriasis|Psoriatic Arthritis October 1, 2012 Phase 3
NCT00866359 Celgene Corporation Behcet Syndrome October 2009 Phase 2
NCT01041625 Virginia Clinical Research, Inc.|Celgene Corporation Lichen Planus February 2010 Phase 2
NCT02558361 University of South Florida Psoriatic Arthritis April 2016 Phase 4
NCT02289417 Celgene Ulcerative Colitis December 10, 2014 Phase 2
NCT01583374 Celgene Ankylosing Spondyloarthritis May 2, 2012 Phase 3
NCT00944658 Imperial College London|Celgene Corporation Ankylosing Spondylitis August 2009 Phase 2
NCT02695212 Florida Academic Dermatology Centers Hidradenitis Suppurativa July 2016 Phase 2
NCT01285310 Celgene Corporation|Celgene Rheumatoid Arthritis December 2010 Phase 2
NCT01988103 Celgene Corporation Psoriasis;|Psoriatic Arthritis;|Psoriasis Arthropatica July 2013 Phase 2
NCT03160248 Technische Universität München|Celgene Corporation Nummular Eczema|Eczema|Dermatitis Eczema|Nummular Dermatitis June 2017 Phase 2
NCT00889421 Oregon Health and Science University|Celgene Corporation Uveitis November 2009 Phase 1|Phase 2
NCT01172938 Celgene Psoriatic Arthritis June 2010 Phase 3
NCT01212757 Celgene Psoriatic Arthritis September 27, 2010 Phase 3
NCT03049267 M.B.A. van Doorn|Celgene|Erasmus Medical Center Hidradenitis Suppurativa February 2, 2017 Phase 2
NCT01194219 Celgene Plaque Psoriasis September 2010 Phase 3
NCT02684123 Icahn School of Medicine at Mount Sinai Alopecia Areata February 2016
NCT00997581 Dartmouth-Hitchcock Medical Center|Celgene Corporation Acute Gout April 2010 Phase 2
NCT02412644 Psoriasis Treatment Center of Central New Jersey|Celgene Plaque Psoriasis April 2015 Phase 4
NCT02777554 Celgene Healthy Volunteers August 17, 2016 Phase 1
NCT02087943 Celgene Dermatitis, Atopic Dermatitis June 2014 Phase 2
NCT01045551 Julian M. Mackay-Wiggan|Celgene Corporation|Columbia University Erythematotelangiectatic Rosacea|Papulopustular Rosacea June 2010 Phase 2
NCT01200472 University of Erlangen-Nürnberg Medical School|Celgene Corporation Erosive Osteoarthritis of the Hand August 2010 Phase 2
NCT01204138 Stanford University|Celgene Corporation Arthritis, Rheumatoid September 2010 Phase 2
NCT03036995 Centre Hospitalier Universitaire de Nice Vitiligo March 20, 2017 Phase 2
NCT01393158 Oregon Health and Science University|Celgene Corporation Atopic Dermatitis
NCT02802735 Celgene Corporation Pharmacokinetics June 2016 Phase 1
NCT03175549 The Scripps Research Institute|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Alcohol Use Disorder July 2017 Phase 2
NCT03146247 Diamant Thaci|University of Luebeck Moderate to Severe Plaque Psoriasis June 15, 2017 Phase 4
NCT03123016 Icahn School of Medicine at Mount Sinai|Celgene Vitiligo April 14, 2017 Phase 2
NCT02954081 Prof. Kristian Reich|Sciderm GmbH Psoriasis January 2017
NCT00773734 Celgene Corporation Psoriasis|Plaque-type Psoriasis September 2008 Phase 2
NCT03022617 University of Alabama at Birmingham|Celgene Psoriatic Nail|Psoriasis Vulgaris|Psoriasis January 2017 Phase 4
NCT03168256 Can-Fite BioPharma Plaque Psoriasis February 2018 Phase 3
NCT02963779 Eli Lilly and Company Healthy December 2016 Phase 1
NCT00606450 Celgene Corporation|Celgene Psoriasis April 2006 Phase 2
NCT00701311 Kenneth Peters, MD|Celgene Corporation|William Beaumont Hospitals Prostatitis|Chronic Prostatitis With Chronic Pelvic Pain Syndrome June 2008 Phase 2
NCT00814632 Kenneth Peters, MD|Celgene Corporation|William Beaumont Hospitals Vulvodynia December 2008 Phase 2
NCT00456092 Celgene Corporation|Celgene Psoriatic Arthritis January 2009 Phase 2
NCT00869089 University Hospitals Cleveland Medical Center|Celgene Corporation Prurigo Nodularis September 2008 Phase 2
NCT00708916 New York University School of Medicine|Celgene Corporation Discoid Lupus Erythematosus June 2008 Phase 1|Phase 2
NCT00604682 Celgene Corporation Psoriasis January 2005 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[1]

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

Animal Administration
[1][2]

Apremilast is prepared in 0.5 % carboxymethylcellulose and 0.25 % Tween 80 (Mice)[1].

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.
Rat[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
Molecular Weight

460.5

Formula

C₂₂H₂₄N₂O₇S

CAS No.

608141-41-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.87%

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Apremilast
Cat. No.:
HY-12085
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