153559-76-3
中文名稱
6-[1-(5,6,7,8-四氫-3,5,5,8,8-五甲基-2-萘基)環(huán)丙基]-3-吡啶羧酸
英文名稱
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID
CAS
153559-76-3
分子式
C24H29NO2
分子量
363.49
MOL 文件
153559-76-3.mol
更新日期
2023/03/20 15:41:27
153559-76-3 結(jié)構(gòu)式
基本信息
中文別名
6-[1-(5,6,7,8-四氫-3,5,5,8,8-五甲基-2-萘基)環(huán)丙基]-3-吡啶羧酸 英文別名
LG 268CD 3127
lg100268
ALRT 268
LGD 1268
AGN 192620
LGD 100268
hthalenyl)cyclopropyl)-
3-pyridinecarboxylicacid,6-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-nap
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID
物理化學(xué)性質(zhì)
熔點(diǎn)275-277°C
沸點(diǎn)487.0±33.0 °C(Predicted)
密度1.115±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C
儲(chǔ)存條件-20°C冷凍
溶解度DMSO：≥5mg/mL（加熱）
酸度系數(shù)(pKa)2.35±0.10(Predicted)
形態(tài)粉末
顏色白色至米色
常見(jiàn)問(wèn)題列表
生物活性
LG100268 (LG268) 是一種有效的、選擇性的，具有口服活性的視黃素X受體 (RXR) 激動(dòng)劑，對(duì) RXR-α，RXR-β，和RXR-γ 的 EC50 值分別為 4 nM、3 nM、4 nM。LG100268 顯示對(duì) RXR 的選擇性優(yōu)于 RAR (1000 倍)，?對(duì) RXR-α，RXR-β，和 RXR-γ 的 Ki 值分別為 3.4 nM，6.2 nM 和 9.2 nM。LG100268 激活 RXR 同源二聚體，誘導(dǎo)轉(zhuǎn)錄激活。LG100268 可用于肺癌的研究。體外研究
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. |
體內(nèi)研究
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. |