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Apremilast

Catalog No. T2923 CAS 608141-41-9

Synonyms: CC-10004

Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.

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Apremilast, CAS 608141-41-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 58.00
25 mg	In stock	$ 71.00
100 mg	In stock	$ 98.00
200 mg	In stock	$ 158.00
500 mg	In stock	$ 266.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.21%

Purity: 98.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.
Targets&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[1].
Cell Research	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].

Synonyms	CC-10004
Molecular Weight	460.5
Formula	C22H24N2O7S
CAS No.	608141-41-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 92 mg/mL (199.78 mM)

References and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Drug Repurposing Compound Library Apoptosis Compound Library Immuno-Oncology Compound Library Bioactive Compound Library

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Keywords

Apremilast 608141-41-9 Apoptosis Metabolism TNF PDE TNFR orally TNF Receptor nucleotide inhibit lipopolysaccharide LPS phosphodiesterase CC 10004 PBMC Tumor Necrosis Factor Receptor CC10004 cyclic Phosphodiesterase (PDE) available CC-10004 Inhibitor type-4 inhibitor

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