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CAS RN: 608141-41-9 | 产品编码: A3669
Apremilast
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| 产品编码 | A3669 |
| 纯度/分析方法 | >98.0%(T)(HPLC) |
| 分子式/分子量 | C__2__2H__2__4N__2O__7S = 460.50 |
| 外观与形状（20°C） | 固体 |
| 储存温度 | 冷藏 (0-10°C) |
| 储存在惰性气体下 | 存放于惰性气体之中 |
| 应避免的情况 | 空气,加热 |
| 包装和容器 | 1G-Glass Bottle with Plastic Insert （查看图片） |
| CAS RN | 608141-41-9 |
| Reaxys-RN | 12446985 |
| MDL编号 | MFCD18782607 |
技术规格
| Appearance | White to Light yellow powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Purity(Volumetric Analysis) | min. 98.0 % |
| Melting point | 155.0 to 159.0 °C |
| Specific rotation | +26.0 to +30.0 deg(C=2, CHCl3) |
| NMR | confirm to structure |
物性（参考值）
| 熔点 | 157 °C |
| 水溶性 | 不溶 |
| 溶解性（可溶于） | 四氢呋喃, 丙酮, 二氯甲烷 |
| 溶解性（不溶于） | 甲苯 |
GHS
| 象形图 |
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| 信号词 | Warning |
| 危险性说明 | H361 : Suspected of damaging fertility or the unborn child. |
| 防范说明 | P501 : Dispose of contents/ container to an approved waste disposal plant. P202 : Do not handle until all safety precautions have been read and understood. P201 : Obtain special instructions before use. P280 : Wear protective gloves/ protective clothing/ eye protection/ face protection. P308 + P313 : IF exposed or concerned: Get medical advice/ attention. P405 : Store locked up. |
相关法规
运输信息
| HS编码* | 2930.90-900 |
应用
Apremilast: A cAMP Phosphodiesterase-4 Inhibitor
Phosphodiesterase-4 (PDE4), primarily found in immune, epithelial and brain cells, is an intracellular non-receptor enzyme that modulates inflammation and epithelial integrity. PDE4 participates in the regulation of the inflammatory response by degrading adenosine 3', 5'-cyclicmonophosphate (cAMP) [A2381, A2112 (Na salt)], a key second messenger. Inhibition of PDE4 increases intracellular cAMP levels, resulting in a decrease in pro-inflammatory mediators and an increase in anti-inflammatory mediators. Apremilast is an oral, small molecule inhibitor of PDE4 that is specific for cAMP. PDE4 inhibition results in increased intracellular cAMP levels. In clinical use, apremilast is approved for the treatment of inflammatory diseases, psoriasis and psoriatic arthritis. (The product is for research purpose only.)
References
- Discovery of (S)-N-{2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide (Apremilast Apremilast ), a Potent and Orally Active Phosphodiesterase 4 and Tumor Necrosis Factor-α Inhibitor
- Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis
- Apremilast mechanism of action and application to psoriasis and psoriatic arthritis (a review)
- Analytical Methods for Determination of Apremilast from Bulk, Dosage Form and Biological Fluids: A Critical Review
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