Name: Apremilast
Brand: Selleck Chemicals
SKU: S8034
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Other PDE Inhibitors	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Cilomilast Mardepodect (PF-2545920) Deltarasin PF-8380 Enpp-1-IN-1 Ibudilast BRL-50481

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.600mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 92 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.150mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	460.5	Formula	C₂₂H₂₄N₂O₇S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	608141-41-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CC-10004			SMILES	CCOC1=C(C=CC(=C1)C(CS(=O)(=O)C)N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)C)OC

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	PDE4 74 nM TNF-α 77 nM
In vitro	Apremilast is more potent for inhibition of PDE4 compared with cAMP or cGMP hydrolysing enzymes from other PDE families. This compound displays a broad pattern of anti-inflammatory activity in a variety of cell types, inhibits TNF-α, IL-12 and IL-23 production, as well as NK and keratinocyte responses. It is found to inhibit the zymosan-induced PMN production of IL-8 with IC50 of 94 nM. This chemical inhibits fMLF-induced PMN CD18 and CD11b expression with IC50 of 390 nM and 74 nM, respectively, and inhibits fMLF-induced adhesion of PMN to HUVECs with IC50 of 150 nM. It inhibits keratinocyte TNF-αproduction, with no effect on keratinocyte cell viability as measured by intracellular ATP levels. .
Kinase Assay	PDE4 inhibitory activity
Kinase Assay	Cells (1×10⁹) are washed in PBS and lysed in cold homogenization buffer (20 mM Tris-HCl, pH 7.1, 3 mM 2-mercaptoethanol, 1 mM MgCl₂, 0.1 mM EGTA, 1 μM PMSF, 1 μg/mL leupeptin). Following homogenization in a Dounce homogenizer the supematant is collected by centrifugation and loaded onto a Sephacryl S-200 column equilibrated in homogenization buffer. PDE is eluted in homogenization buffer and the rolipram sensitive fractions pooled and stored in aliquots. Enzyme activity is assayed in 50 mM Tris- HCl, pH 7.5, 5 mM MgCl₂ and 1 μM cAMP (of which 1% is³H cAMP) in the presence of varying concentrations of inhibitors. The amount of extract used is pre-determined to ensure that reactions are within the linear range and consumed lessthan15%of the total substrate. Reactions are performed at 30°C for 30 min and terminated by boiling for 2 min. The samples are then chilled and treated with snake 'venom (1mg/mL) at 30 °C for 15 min. Unused substrate is removed by incubation with 200 μL AG1-X8 resin for 15 min. Samples are then spun at 3000 rpm for 5 min and 50 μL of the aqueous phase taken for counting. Eachdata point is carried out in duplicate with activity expressed as percentage of control. IC50 is determined from dose response curves derived from three independent experiments.
In vivo	Apremilast is stable in the presence of human microsomes (t1/2 > 60 min). It is 90% protein bound in human plasma. Oral and intravenous administration of this compound in female rats showed that it have good pharmacokinetics with low clearance, a moderate volume of distribution, and a 64% oral bioavailability. In a LPS-induced TNF-αinhibition model in rats, examined the TNF-α inhibitory ability of this compound in vivo, and the ED50 is determined to be 0.03 mg/kg. In another LPS-induced neutrophilia model in rats, this compound exhibited an ED50 range from 0.3 mg/kg to 0.9 mg/kg.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19256507/ [2] https://pubmed.ncbi.nlm.nih.gov/9873600/ [3] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2829210 [4] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2911898

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-12-01)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05767047	RECRUITING	Behçet's Disease; Juvenile Psoriatic Arthritis	Amgen	2023-03-23	PHASE3
NCT07029529	RECRUITING	Alcohol Use Disorder	Yale University	2026-05-12	PHASE2
NCT07352566	NOT_YET_RECRUITING	Psoriasis; Atopic Dermatitis	University of California, San Francisco	2026-08-01	PHASE4
NCT04528082	RECRUITING	Behçet Disease	Amgen	2021-09-09	PHASE3
NCT05703685	RECRUITING	Depression	National Institute of Mental Health (NIMH)	2023-06-22	PHASE1
NCT04488081	ACTIVE_NOT_RECRUITING	COVID-19	QuantumLeap Healthcare Collaborative	2020-07-31	PHASE2

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Apremilast PDE inhibitor

Chemical Structure

Molecular Weight: 460.5