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Apremilast-d5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Apremilast-d5图片
规格:98%
分子量:465.5
包装与价格:
包装价格(元)
500ug电议
1mg电议

产品介绍
Apremilast D5 (CC-10004 D5) 是一种氘标记的 Apremilast。
货号:ajcx21694
CAS:1258597-47-5
分子式:C22H19D5N2O7S
分子量:465.5
溶解度:Acetonitrile: soluble,Methanol: soluble
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Apremilast-d5is 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 IC50value of 74 nM when tested in U937 cell lysates with 1 mM cAMP.1,2It is orally active, significantly decreasing epidermal thickness and the epithelial cell proliferation index in a mouse model of psoriasis.2Apremilast reduces both TNF-α and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease.3It 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)