HLY78 是 Lycorine (HY-N0288) 衍生物，是一种有效的Wnt/β-catenin信号通路的激活剂。HLY78 靶向于 Axin 的 DIX 结构域，促进 Axin-LRP6 的关联，从而促进 LRP6 磷酸化 (LRP6 phosphorylation) 和 Wnt 信号转导。HLY78 可用于蛛网膜下腔出血 (SAH) 的研究。
| 生物活性 | HLY78, aLycorine(HY-N0288) derivative, is a potent activator of theWnt/β-cateninsignaling pathway. HLY78 targets the DIX domain of Axin and promotes the Axin-LRP6 (lipoprotein receptor-related protein 6) association, thus promotingLRP6 phosphorylationandWntsignal transduction. HLY78 can be used for subarachnoid hemorrhage (SAH) research[1][2][3]. |
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体外研究
(In Vitro) | HLY78 inhibitsapoptosisin tumor cells and embryonic cells caused by carbon ion radiation through activation of the Wnt/β-catenin pathway[2].
HLY78 (20 μM, 0-48 h) significantly increases the colony formation ability by 2.78-fold and 2.88-fold for HGC-27 and AGS cells compared with the controls[3].
HLY78 (20 μM, 0-48 h) elevates the migration ability of HGC-27 and AGS cells[3].
HLY78 significantly increases TNKS expression, which is ameliorated byDihydroartemisinin(HY-N0176)[3].
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体内研究
(In Vivo) | HLY78 (0-1.8 mg/kg, Intranasal injection, once) attenuates neuronal apoptosis and improves neurological deficits through the LRP6/GSK3β/β-catenin signaling pathway after SAH (subarachnoid hemorrhage) in rats[2].
| Animal Model: | Adult male Sprague-Dawley rats (280-310 g, n=9/group, SAH model)[2] | | Dosage: | 0, 0.2, 0.6, and 1.8 mg/kg | | Administration: | Intranasal injection, once, at 1 h post-SAH (subarachnoid hemorrhage) | | Result: | Significantly attenuated the short-term and long-term neurobehavioral deficits, as well as the neuronal apoptosis after SAH at 0.6 mg/kg. Successfully delivered into the brain via intranasal administration at 0.6 mg/kg and was sufficient to significantly increase the phosphorylation of LRP6. Reversed the changes of the Bcl-2, Bax, and cleaved caspase 3 levels. |
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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 | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 26 mg/mL(97.26 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.7408 mL | 18.7042 mL | 37.4083 mL | | 5 mM | 0.7482 mL | 3.7408 mL | 7.4817 mL | | 10 mM | 0.3741 mL | 1.8704 mL | 3.7408 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。 |
