6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸
| 中文名称 | 6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸 |
|---|---|
| 中文同义词 | 6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸;6-[1-(3,5,5,8,8-五甲基-5,6,7,8-四氢-2-萘基)环丙基]烟酸;化合物 T19703 |
| 英文名称 | 6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID |
| 英文同义词 | 2-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)cyclopropyl]pyridine-5-carboxylic acid;6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID;6-[1-(3,5,5,8,8-PentaMethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid;3-Pyridinecarboxylicacid,6-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentaMethyl-2-naphthalenyl)cyclopropyl]-;3-pyridinecarboxylicacid,6-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-nap;hthalenyl)cyclopropyl)-;lg100268;6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID (FOR R&D ONLY) |
| CAS号 | 153559-76-3 |
| 分子式 | C24H29NO2 |
| 分子量 | 363.49 |
| EINECS号 | |
| 相关类别 | Intermediates & Fine Chemicals;Pharmaceuticals;Retinoids |
| Mol文件 | 153559-76-3.mol |
| 结构式 | ![6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸 结构式](CAS/GIF/153559-76-3.gif) |
6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸 性质
| 熔点 | 275-277°C |
|---|---|
| 沸点 | 487.0±33.0 °C(Predicted) |
| 密度 | 1.115±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | DMSO：≥5mg/mL（加热） |
| 酸度系数(pKa) | 2.35±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
LG100268 (LG268) 是一种有效的、选择性的，具有口服活性的视黄素X受体 (RXR) 激动剂，对 RXR-α，RXR-β，和RXR-γ 的 EC50 值分别为 4 nM、3 nM、4 nM。LG100268 显示对 RXR 的选择性优于 RAR (1000 倍)， 对 RXR-α，RXR-β，和 RXR-γ 的 Ki 值分别为 3.4 nM，6.2 nM 和 9.2 nM。LG100268 激活 RXR 同源二聚体，诱导转录激活。LG100268 可用于肺癌的研究。
LG100268 (100 nM-1 μM; 24 hours) shows a downregulation of CSF3 and a 2.5-fold decrease of CXCL2 and IL-1β mRNA expression in RAW264.7 cells.
Cell Viability Assay
| Cell Line: | RAW264.7 cells |
| Concentration: | 100 nM-1 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased LPS induced cytokine mRNA levels. |
LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) combines with C/P presents a more markedly reduced average tumor burden than LG268 or C/P alone. The combination establish a reduced lung tumors, which represents a reduction of 82% (vs. 59%-67% with the single drugs) in comparison with the controls.
| Animal Model: | A/J mice |
| Dosage: | 50 mg/kg (Combines with carboplatin (50 mg/kg i.p.) starts 1 week after the LG268 treatment diet) |
| Administration: | Oral diet; once daily; 7 weeks |
| Result: | Decreased lung tumors growth significantly in mice. |
安全信息
| WGK Germany | 3 |
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-15340 | LG100268 | 1 mg | 454元 | |
| 2024/04/30 | HY-15340 | 6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸 LG100268 | 153559-76-3 | 5mg | 1000元 |