楝酰胺
| 中文名称 | 楝酰胺 |
|---|---|
| 中文同义词 | 洛克米兰酰胺;楝酰胺;(1R,2R,3S,3AR,8BS)-1,8B-二羟基-6,8-二甲氧基-3A-(4-甲氧基苯基)-N,N-二甲基-3-苯基-2,3,3A,8B-四氢-1H-环戊二烯并[B]苯并呋喃-2-甲酰胺 |
| 英文名称 | ROCAGLAMIDE |
| 英文同义词 | ROCAGLAMIDE;(1R)-2,3,3a,8b-Tetrahydro-1α,8bβ-dihydroxy-6,8-dimethoxy-3aβ-(4-methoxyphenyl)-N,N-dimethyl-3β-phenyl-1H-cyclopenta[b]benzofuran-2α-carboxamide;(1R)-N,N-Dimethyl-1α,8bβ-dihydroxy-3β-phenyl-3aβ-(4-methoxyphenyl)-6,8-dimethoxy-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-2α-carboxamide;2,3,3a,8b-Tetrahydro-1α,8bβ-dihydroxy-6,8-dimethoxy-3aβ-(4-methoxyphenyl)-N,N-dimethyl-3β-phenyl-1H-cyclopenta[b]benzofuran-2α-carboxamide;2,3,3a,8b-Tetrahydro-N,N-dimethyl-1α,8bβ-dihydroxy-6,8-dimethoxy-3β-phenyl-3aβ-(4-methoxyphenyl)-1H-cyclopenta[b]benzofuran-2α-carboxamide;N,N-Dimethyl-1α,8bβ-dihydroxy-6,8-dimethoxy-3β-phenyl-3aβ-(4-methoxyphenyl)-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-2α-carboxamide;(1R,2R,3S,3aR,8bS)-2,3,3a,8b-Tetrahydro-1,8b-dihydroxy-6,8-dimethoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-1H-cyclopenta[b]benzofuran-2-carboxamide;NSC 326408 |
| CAS号 | 84573-16-0 |
| 分子式 | C29H31NO7 |
| 分子量 | 505.56 |
| EINECS号 | |
| 相关类别 | 生物碱 |
| Mol文件 | 84573-16-0.mol |
| 结构式 |  |
楝酰胺 性质
| 熔点 | 117-118 °C |
|---|---|
| 沸点 | 667.3±55.0 °C(Predicted) |
| 密度 | 1.321±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 溶于DMSO或乙醇 |
| 形态 | 膜状 |
| 酸度系数(pKa) | 11.70±0.70(Predicted) |
| 颜色 | 无色 |
| 稳定性 | 从购买之日起 2 年内保持稳定。 DMSO 或乙醇溶液可在 -20°C 下保存长达 1 个月。避免暴露在光线和湿气中。 |
(2) 楝酰胺的直接作用靶标为ULK1，ULK1是参与自噬发生的重要激酶。Rocaglamide (Roc-A) 是从 Aglaia 中分离出来，可用于咳嗽，受伤，哮喘和炎症性皮肤病。Rocaglamide 是 T 细胞中一种有效的 NF-κB 活化抑制剂。Rocaglamide 是一种有效的选择性热休克因子 1 (HSF1) 活化抑制剂，IC50 约为 50 nM。Rocaglamide 还抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还具有抗癌特性。
|
HSF1 50 nM (IC 50 ) |
Rocaglamide enhances TRAIL-induced apoptosis in resistant HCC cells. Treatment with Rocaglamide alone leads to apoptosis in 9% HepG2 and 11% Huh-7 cells and treatment with TRAIL induces apoptosis in 16% HepG2 and 17% Huh-7 cells. However, the combination of Rocaglamide and TRAIL induces apoptosis in 55% HepG2 and 57% Huh-7 cells, which is evidently more than an additive effect. A similar result is obtained by measurement of cell viability using crystal violet staining. Rocaglamide has the potential to sensitize highly chemoresistant HepG2 and Huh-7 cells to TRAIL-based therapy.
Tumor volumes in the Rocaglamide-treated group are 45±12% compared with the control group. Rocaglamide significantly suppresses tumor growth compared with that in the control group. Treatment with Rocaglamide does not lead to any reduction in body weight and no apparent signs of toxicity are observed in the mice during the treatment, suggesting that Rocaglamide is generally tolerated well.
安全信息
| WGK Germany | 3 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19356 | 楝酰胺 Rocaglamide | 84573-16-0 | 500μg | 1280元 |
| 2024/01/25 | HY-19356 | 楝酰胺 Rocaglamide | 84573-16-0 | 1mg | 2050元 |