Aldometanib (LXY-05-029) 是一种醛缩酶抑制剂。Aldometanib 可以激活溶酶体腺苷-磷酸活化蛋白激酶AMPK并降低血糖。Aldometanib 可用于代谢稳态的研究。
| 生物活性 | Aldometanib (LXY-05-029) is an orally activealdolaseinhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis[1]. |
体外研究
(In Vitro) | Aldometanib (0-1000 nM; 2 h) activates AMPK by preventing aldolase from binding to FBP to engender a pseudo-starvation signal[1].
Western Blot Analysis[1] | Cell Line: | Mouse primary hepatocytes, MEFs cells | | Concentration: | 0-1000 nM | | Incubation Time: | 2 h | | Result: | Activated AMPK in mouse embryonic fibroblasts (MEFs) and mouse primary hepatocytes cells. |
Immunofluorescence[1] | Cell Line: | MEFs cells | | Concentration: | 5 nM | | Incubation Time: | 2 h | | Result: | Inhibited TRPVs and induces AXIN lysosomal translocation. |
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体内研究
(In Vivo) | Aldometanib (oral; 0-10 mpk) reduces blood glucose in lean mice[1].
Aldometanib (oral; 2-10 mpk; twice daily; for a week) reduces blood glucose and alleviates fatty liver in obese hyperglycaemic mice[1].
Aldometanib alleviates fatty liver and nonalcoholic steatohepatitis[1].
Aldometanib (oral; 2mpk; twice-daily; for a month) alleviates liver fibrosis in NASH mice[1].
Aldometanib (oral; 0-50 μM; 0-50 days) extends lifespan inC. elegansvia the lysosomal pathway[1].
| Animal Model: | Lean mice[1] | | Dosage: | 0-10 mpk | | Administration: | Oral | | Result: | Decreased fasting blood glucose and improved glucose tolerance, promoted muscular TBC1D1 phosphorylation and glucose uptake. |
| Animal Model: | Obese hyperglycaemic mice[1] | | Dosage: | 2-10 mpk | | Administration: | Oral, twice daily, for a week | | Result: | Decreased blood glucose, lowered blood glucose in a muscular AMPK-dependent manner reduced hepatic TAG, improved insulin sensitivity, increased glucose disposal rates, inhibited TAG synthesis in liver and primary hepatocytes, decreased fat mass. |
| Animal Model: | NASH mice[1] | | Dosage: | 2 mpk | | Administration: | Oral, twice-daily, for a month | | Result: | Decreased histological scores used to describe the features of NASH, reduced apoptosis rate of hepatic cells, inhibited inflammatory responses in the liver of NASH mice and improved glucose tolerance of NASH mice. |
| Animal Model: | C. elegans[1] | | Dosage: | 0-50 μM | | Administration: | Oral, 0-50 days | | Result: | Promoted oxidative stress resistance and mitochondrial functions inC. elegans. |
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 100 μg/mL | | Administration: | Oral | | Result: | Extended lifespan, elevated NAD＋levels and mitochondrial oxidative respiration, rejuvenated muscle function in aged mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(168.51 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.6851 mL | 8.4253 mL | 16.8506 mL | | 5 mM | 0.3370 mL | 1.6851 mL | 3.3701 mL | | 10 mM | 0.1685 mL | 0.8425 mL | 1.6851 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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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