Cat. No.: HY-12085

Apremilast

(Synonyms: CC-10004)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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.

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Pureté: 99.79%
CAS No.: 608141-41-9
Formule: C₂₂H₂₄N₂O₇S
Masse moléculaire:460.50

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Apremilast Chemical Structure

CAS No.: 608141-41-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PDE4

74 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Voir tous les produits spécifiques à Isoform TNF Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	0.077 μM Compound: 1S	Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay	[PMID: 19256507]
Sf9	IC₅₀	21 nM Compound: 30	Inhibition of recombinant human His6-tagged PDE4D UCR2 deletion mutant catalytic domain expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yea Inhibition of recombinant human His6-tagged PDE4D UCR2 deletion mutant catalytic domain expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yea	[PMID: 31013090]
Sf9	IC₅₀	23 nM Compound: 30	Inhibition of recombinant human His6-tagged PDE4D3 UCR1 S54D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvat Inhibition of recombinant human His6-tagged PDE4D3 UCR1 S54D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvat	[PMID: 31013090]
Sf9	IC₅₀	24 nM Compound: 30	Inhibition of recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva Inhibition of recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva	[PMID: 31013090]
Sf9	IC₅₀	26 nM Compound: 30	Inhibition of recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva Inhibition of recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva	[PMID: 31013090]
Sf9	IC₅₀	32 nM Compound: 30	Inhibition of recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by ye Inhibition of recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by ye	[PMID: 31013090]
Sf9	IC₅₀	35 nM Compound: 30	Inhibition of recombinant human His6-tagged PDE4D2 expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvate kinase/lactate Inhibition of recombinant human His6-tagged PDE4D2 expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvate kinase/lactate	[PMID: 31013090]

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].

MedChemExpress (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 (C_max) 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]

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 608141-41-9
Appearance Solid
Masse moléculaire 460.50
Formule C₂₂H₂₄N₂O₇S
Color White to light yellow
SMILES

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

CC-10004
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (10)

All RT-PCRELISACell Imaging/StainingFlow CytometryWB

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Journal Impact Factor

Phytomedicine

Syringin inhibits the crosstalk between macrophages and fibroblast-like synoviocytes to treat rheumatoid arthritis via PDE4. [Abstract]

2025 Mar:138:156401. PMID: 39842374
Int J Mol Med

Apremilast prevents IL‑17‑induced cellular senescence in ATDC5 chondrocytes mediated by SIRT1. [Abstract]

2021 Mar;47(3):12. PMID: 33448323

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevented IL-17-induced expression of pro-inflammatory cytokines in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (0.5 and 1 µM) for 24 h.

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevents IL-17-induced secretions of pro-inflammatory cytokines in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (0.5 and 1 µM) for 24 h.

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevented IL-17-induced production of ROS in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (0.5 and 1 µM) for 24 h. Production of ROS was measured using DCFH-DA staining (magnification, ×10). ROS, reactive oxygen species; IL, interleukin; DCFH-DA, 2,7-dichlorodihydrofluorescein diacetate.

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevented IL-17-induced cellular senescence in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (1 µM) for 7 days. Cellular senescence was measured using SA-β-gal staining. IL, interleukin; SA-β-gal, senescence-associated-β-galactosidase.

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevented IL-17-induced cell cycle arrest in the G0/G1 phase in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (1 µM) for 7 days. The cell cycle was assayed using flow cytometry. G0/G1 phase, G2/M phase, and S phase of cells were measured.

Apremilast purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Mar;47(3):12. [Abstract]

Apremilast prevented IL-17-induced expression of p21 and PAI-1 in mouse ATDC5 chondrocytes. Cells were treated with IL-17 (10 ng/ml) in the presence or absence of Apremilast (1 µM) for 24 h.
Eur J Pharmacol

A novel phosphodiesterase 4 inhibitor, AA6216, reduces macrophage activity and fibrosis in the lung. [Abstract]

2020 Oct 15:885:173508. PMID: 32858049
J Dermatol Sci

PDE4 inhibition by difamilast regulates filaggrin and loricrin expression via keratinocyte proline-rich protein in human keratinocytes. [Abstract]

2023 May;110(2):61-68. PMID: 37156706
J Dermatol Sci

Cyto/chemokine profile of in vitro scratched keratinocyte model: Implications of significant upregulation of CCL20, CXCL8 and IL36G in Koebner phenomenon. [Abstract]

2019 Apr;94(1):244-251. PMID: 31010609
Neuroscience

Apremilast-mediated protection against Aβ-induced cytotoxicity correlates with PI3K/Akt pathway activation. [Abstract]

2026 Feb 16:595:20-27. PMID: 41443295
Biochem Biophys Rep

The phosphodiesterase 4 inhibitor AA6216 suppresses activity of fibrosis-specific macrophages. [Abstract]

2021 Aug 28:28:101118. PMID: 34485715
Res Sq

FDA-approved PDE4 inhibitors alleviate the dominant toxicity of ALS-FTD-associated CHCHD10S59L by reducing the PINK1/Parkin pathway. [Abstract]

2024 Sep 10:rs.3.rs-4870330. PMID: 39315251
bioRxiv

FDA-approved PDE4 inhibitors reduce the dominant toxicity of ALS-FTD-associated CHCHD10 S59L. [Abstract]

2024 Jun 6:2024.06.04.597429. PMID: 38895204
Heinrich Heine University Dusseldorf

2022 May.

Solvant et solubilité

In Vitro:

DMSO : 44 mg/mL (95.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/0.5% Tween-80 in Saline water

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

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].

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Perez-Aso M, et al. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 2015 Sep 15;17:249. [Content Brief]

[2]. Chen LG, et al. Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study. J Chromatogr Sci. 2016 Sep;54(8):1336-40. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1716 mL	10.8578 mL	21.7155 mL	54.2888 mL
	5 mM	0.4343 mL	2.1716 mL	4.3431 mL	10.8578 mL
	10 mM	0.2172 mL	1.0858 mL	2.1716 mL	5.4289 mL
	15 mM	0.1448 mL	0.7239 mL	1.4477 mL	3.6193 mL
	20 mM	0.1086 mL	0.5429 mL	1.0858 mL	2.7144 mL
	25 mM	0.0869 mL	0.4343 mL	0.8686 mL	2.1716 mL
	30 mM	0.0724 mL	0.3619 mL	0.7239 mL	1.8096 mL
	40 mM	0.0543 mL	0.2714 mL	0.5429 mL	1.3572 mL
	50 mM	0.0434 mL	0.2172 mL	0.4343 mL	1.0858 mL
	60 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9048 mL
	80 mM	0.0271 mL	0.1357 mL	0.2714 mL	0.6786 mL

Apremilast

10 Cited Publications

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Apremilast

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Publications Citing Use of MedChemExpress (MCE) Apremilast

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)

Voir tous les produits spécifiques à Isoform TNF Receptor

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Apremilast Related Classifications

HY-12085 Related Classifications