GSK3987 是一种广泛的LXRα/β激动剂，EC50分别为 50 nM 和 40 nM。GSK3987 增加 ABCA1 和 SREBP-1c 蛋白的表达。GSK3987 诱导细胞胆固醇流出和甘油三酯的积累。
| 生物活性 | GSK3987 is a panLXRα/βagonist withEC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellularcholesterolefflux and triglyceride accumulation[1]. |
| IC50& Target | EC50: 50 nM (LXRα); 40 nM (LXRβ)[1] |
体外研究
(In Vitro) | GSK3987 (compound 4) shows activity with EC50s of 0.08 μM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1].
GSK3987 (30, 100, 300, 1000 nM) increases the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner in primary human macrophages[1].
GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner[1].
RT-PCR[1] | Cell Line: | HepG2 cells | | Concentration: | 6-1500 nM | | Incubation Time: | | | Result: | Increased the expression of SREBP-1c and induced triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(260.13 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | | 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | | 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
