| 货号 | 18502-25mg |
| 描述 | 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.1,2 It is orally active, significantly decreasing epidermal thickness and epithelial cell proliferation index in a mouse model of psoriasis.2 Apremilast reduces both TNF-α and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease.3 It also blocks spontaneous production of TNF-α from human rheumatoid synovial cells and improves clinical score in mouse models of arthritis.4 |
| 别名 | CC-10004; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Man, H.W.,Schafer, P.,Wong, L.M., et al. Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor. Journal of Medicinal Chemistry 52(6), 1522-1524 (2009). 2.Schafer, P.H.,Parton, A.,Gandhi, A.K., et al. Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis. British Journal of Pharmacology 159(4), 842-855 (2010). 3.Gordon, J.C.,Prothero, J.D.,Thornton, C.A., et al. CC-10004 but not thalidomide or lenalidomide inhibits lamina propria mononuclear cell TNF-α and MMP-3 production in patients with inflammatory bowel disease. J.Crohns.Colitis. 3(3), 175-182 (2009). 4.McCann, F.E.,Palfreeman, A.C.,Andrews, M., et al. Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis. Arthritis Research & Therapy 12(3), (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 460.5 |
| 分子式 | C22H24N2O7S |
| CAS号 | 608141-41-9 |
| 稳定性 | ≥ 2 years |
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