5300-03-8
5300-03-8 结构式
基本信息
异维A酸杂质4
9-顺式维甲酸
9-顺式视黄酸
9-CIS维甲酸
维A酸EP杂质D
9-顺式视黄醇酸
异维A酸EP杂质D
异维甲酸EP杂质D
9-顺-视黄酸 [干冰运输,需加收额外费用]
物理化学性质
常见问题列表
异维A酸EP杂质D是异维A酸合成过程中产生产生的杂质，又名阿利维甲酸，是治疗皮肤病领域的重要药物，是全反式维甲酸(式II，化学名：3，7-二甲基-9-(2，6，6-三甲基环己烯-1-基)-2E，4E，6E，8E-全反式壬四烯酸)的9-顺异构体。
异维A酸EP杂质D（式I化合物）的制备：在氮气保护下，往反应瓶中加入乙醇2L、全反式维甲酸100g，搅拌，然后升温至50～55℃，加入PdCl289mg。反应1.5h后，经HPLC检测产物纯度为21％。反应液缓慢降温至0～5℃，保温180分钟，抽滤；滤液加入另一干净反应瓶中，继续降温至-10～-6℃，保温20分钟，抽滤，得到产物异维A酸EP杂质D 12.1g，总收率12.1％，HPLC纯度99.60％。以全反式维甲酸为原料，采用钯化合物催化，在普通的工业级有机溶剂中可得到阿利维甲酸。方法操作简便，成本低，条件可控，便于工业生产；经过后处理步骤后，可得到纯度99％以上的阿利维甲酸，产物收率达到12％以上，具有较高的应用价值。
9-cis-Retinoic acid (1-10 μM; 0-5 days; CA 9-22 and NA cells) treatment significantly decreases proliferation in a dose-dependent manner in CA 9-22 and NA cells.
9-cis-Retinoic acid (1 μM; 24 hours) treatment significantly increases PPARγ functional activity by >200% in CA 9-22 and NA aerodigestive cells.
9-cis-Retinoic acid treatment results in the formation of a nuclear PPARγ-RXRα heterodimer supershift complex in CA 9-22 cells.
9-cis-Retinoic acid inhibits proliferation and induces apoptosis in cutaneous T-cell lymphoma (CTCL) in a dose-dependent and time-dependent manner. 9-cis-Retinoic acid also induces G0/G1 cell cycle arrest by downregulation of cyclin D1. 9-cis-Retinoic acid significantly decreases phosphorylation of JAK1, STAT3, and STAT5 and downregulated Bcl-xL and cyclin D1.
Cell Proliferation Assay
| Cell Line: | CA 9-22 and NA cells |
| Concentration: | 1 μM, 10 μM |
| Incubation Time: | 0 day, 1 day, 3 days, 5 days |
| Result: | Significantly decreased proliferation. |
9-cis-Retinoic acid (1 mg/kg; intravenous injection; daily; for 10 days; male C57BL/6J mice) treatment significantly decreases the serum ALT and AST level, alleviates hepatic necrosis of the bile duct ligation (BDL)-mice.
| Animal Model: | Male C57BL/6J mice (6-8 weeks; 19-22 g) treatment with bile duct ligated |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection; daily; for 10 days |
| Result: | Significantly decreased the serum ALT and AST level, alleviated hepatic necrosis. |