An orally active inhibitor of PDE4 with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP; decreases epidermal thickness in a mouse model of psoriasis

Apremilast – 5 mg

Brand:
Cayman
CAS:
608141-41-9
Storage:
-20
UN-No:
Non-Hazardous - /

Apremilast is an inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP.{29958,29960} It is orally active, significantly decreasing epidermal thickness and epithelial cell proliferation index in a mouse model of psoriasis.{29960} Apremilast reduces both TNF-α and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease.{29957} It also blocks spontaneous production of TNF-α from human rheumatoid synovial cells and improves clinical score in mouse models of arthritis.{29959}  

 

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Description

An orally active inhibitor of PDE4 with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP; decreases epidermal thickness in a mouse model of psoriasis, reduces both TNF-α and MMP-3 production in gut cells from patients with IBD, and improves clinical score in mouse models of arthritis

Formal name: N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-acetamide

Synonyms:  CC-10004

Molecular weight: 460.5

CAS: 608141-41-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Gastric Disease|IBS

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