產品屬性：
產品名稱 | Apremilast-d5 |
規格 | 500 μg、1 mg |
貨號 | EY-01Y15877 |
Cas No.: 1258597-47-5
別名: N/A
化學名: N/A
分子式: C22H19D5N2O7S
分子量: 465.5
溶解度: Acetonitrile: soluble,Methanol: soluble
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
Apremilast-d5 is intended for use as an internal standard for the quantification of apremilast by GC- or LC-MS. 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 the 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 the clinical score in mouse models of arthritis.4
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 inhibitorJournal of Medicinal Chemistry52(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 psoriasisBritish Journal of Pharmacology159(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 diseaseJ.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 arthritisArthritis Research & Therapy12(3)(2010)
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