| Bioactivity | 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[1][2]. |
| Target | Ki: 2.7 nM (RXRα) |
| Invitro | 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[1]。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[2]。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[2]。LG101506 (30 and 100 nM; 1-24 h) 诱导 U937 白血病细胞分化[2]。 Western Blot Analysis[2] Cell Line: |
| In Vivo | LG101506 (10 mg/kg; in diet for 16 weeks) 抑制 A/J 小鼠肺癌的发生[2]。 Animal Model: |
| Name | LG101506 |
| CAS | 331248-11-4 |
| Formula | C25H34F2O3 |
| Molar Mass | 420.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gernert DL, et al. Design and synthesis of fluorinated RXR modulators. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5. [2]. Cao M, et al. The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila). 2016 Jan;9(1):105-14. |