Apremilast-d
Cat. No.：YN270650
| 产品名称: | Apremilast-d |
| CAS No.: | 1258597-47-5 |
| Chemical Name: | N-[2-[(1S)-1-[3-(ethoxy-1,1,2,2,2-d5)-4-methoxyphenyl]-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-acetamide |
| Synonyms: | CC-10004-d |
| 分子量: | 465.5 |
| 分子式: | C22H19D5N2O7S |
| SMILES: | O=C1N([C@H](CS(C)(=O)=O)C2=CC(OC([2H])([2H])C([2H])([2H])[2H])=C(OC)C=C2)C(C3=C(NC(C)=O)C=CC=C31)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Apremilast-d5是一种 Apremilast 氘代物。Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂，IC50为 74 nM。Apremilast 抑制脂多糖 (LPS) 释放TNF-α，IC50为 104 nM。 |
| IC50和靶点: | |
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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 inhibitorJ. Med. Chem.52(6),1522-1524(2009)
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 psoriasisBr. J. Pharmacol.159(4),842-855(2010)
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 Colitis3(3),175-182(2009)
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 Res. Ther.12(3),(2010)
