产品描述
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib prevents FBP from binding to v-ATPase-associated aldolase and activates lysosomal AMPK. Aldometanib can be used for the research of metabolic homeostasis [1].

体外活性
Aldometanib (0-1000 nM; 2 h) activates AMPK through 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.

体内活性
Aldometanib (oral; 0-10 mpk) lowers 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 in C. elegans via 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 in C. 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.

Cas No.
T60122

分子式
C27H43Cl2IN2

分子量
593.45

参考文献
[1]Zhang CS, et al. The aldolase inhibitor aldometanib mimics glucose starvation to activate lysosomal AMPK. Nat Metab. 2022 Oct;4(10):1369-1401.

储存和溶解度
( < 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

Note
For research use only .