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编 号：F322480
分子式：C25H34F2O3
分子量：420.53
分子式：C25H34F2O3
分子量：420.53
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CAS No: 331248-11-4
产品详情
生物活性：
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer.
体内研究：
LG101506 (10 mg/kg; in diet for 16 weeks) 抑制 A/J 小鼠肺癌的发生。Animal Model:A/J mice, lung carcinogenesis model
Dosage:40 mg/kg diet or approximately 10 mg/kg body weight
Administration:Oral, for 16 weeks
Result:Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
Animal Model:Male ICR mice
Dosage:30 mg/kg
Administration:Oral (Pharmacokinetic Analysis)
Result:In vivo evaluation of oral exposure of LG101506CompdDose (mg/kg) Oral AUC(0-6 h) (μg?h/mL) Tmax (h)Cmax (μg?h/mL)
LG101506302.09±0.4511.2±0.28
Data collected in male ICR mouse using a dose formulation of the free acid in CMC/SLS/Povidone (30 mg/kg). Timepoints: 1, 3, 8 h (serial sacrifice, n=3/time point).
体外研究：
LG101506 与 BRL 49653 (HY-17386) 协同作用增强 RXR/PPARγ 异源二聚体的激活，EC50 为 3.1 nM。LG101506 (15.6-1000 nM) 以剂量依赖的方式阻断 LPS (HY-D1056) 刺激 RAW264.7 细胞 24 小时内 NO 的产生。LG101506 (100-1000 nM; 24 h) 在 RAW264.7 细胞中抑制 LPS (HY-D1056) 或 TNFα 诱导的炎症通路。LG101506 (30 and 100 nM; 1-24 h) 诱导 U937 白血病细胞分化。
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer.
体内研究：
LG101506 (10 mg/kg; in diet for 16 weeks) 抑制 A/J 小鼠肺癌的发生。Animal Model:A/J mice, lung carcinogenesis model
Dosage:40 mg/kg diet or approximately 10 mg/kg body weight
Administration:Oral, for 16 weeks
Result:Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
Animal Model:Male ICR mice
Dosage:30 mg/kg
Administration:Oral (Pharmacokinetic Analysis)
Result:In vivo evaluation of oral exposure of LG101506CompdDose (mg/kg) Oral AUC(0-6 h) (μg?h/mL) Tmax (h)Cmax (μg?h/mL)
LG101506302.09±0.4511.2±0.28
Data collected in male ICR mouse using a dose formulation of the free acid in CMC/SLS/Povidone (30 mg/kg). Timepoints: 1, 3, 8 h (serial sacrifice, n=3/time point).
体外研究：
LG101506 与 BRL 49653 (HY-17386) 协同作用增强 RXR/PPARγ 异源二聚体的激活，EC50 为 3.1 nM。LG101506 (15.6-1000 nM) 以剂量依赖的方式阻断 LPS (HY-D1056) 刺激 RAW264.7 细胞 24 小时内 NO 的产生。LG101506 (100-1000 nM; 24 h) 在 RAW264.7 细胞中抑制 LPS (HY-D1056) 或 TNFα 诱导的炎症通路。LG101506 (30 and 100 nM; 1-24 h) 诱导 U937 白血病细胞分化。
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