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

生物活性体外研究体内研究 6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸试剂级价格

CAS号:153559-76-3
英文名:6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID
中文名: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
CBNumber:CB6458625
分子式:C24H29NO2
分子量:363.49
MOL File:153559-76-3.mol

6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸化学性质

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 (warmed)
酸度系数(pKa) :2.35±0.10(Predicted)
形态 :powder
颜色 :white to beige

安全信息

WGK Germany :3

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、用途与生产工艺

生物活性 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。

体外研究

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.

体内研究

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.