Apremilast

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. It is orally active, significantly decreasing epidermal thickness and epithelial cell proliferation index in a mouse model of psoriasis. Apremilast reduces both TNF-alpha and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease. It also blocks spontaneous production of TNF-alpha from human rheumatoid synovial cells 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. CAS Number: 608141-41-9. Synonyms: APR, CC-10004. Molecular Formula: C22H24N2O7S. Formula Weight: 460.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 10 mg/ml. lambdamax: 203, 229, 345 nm. SMILES: O=C1N([C@H](CS(C)(=O)=O)C2=CC(OCC)=C(OC)C=C2)C(C3=C(NC(C)=O)C=CC=C31)=O. InChi Code: InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1. InChi Key: IMOZEMNVLZVGJZ-QGZVFWFLSA-N.