Aldometanib

SKU: orb1689820

Description

Aldometanib (LXY-05-029) is an orally bioavailable small molecule that inhibits aldolase, disrupting its interaction with v-ATPase and FBP to activate lysosomal AMPK. This mechanism supports its application in research models investigating metabolic regulation and homeostasis, both in cellular and animal studies.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 2904601-67-6
• MW: 593.46
• Purity: 98.80% (May vary between batches)
• Formula: C₂₇H₄₃Cl₂IN₂
• SMILES: CC1=[N+](C=CN1CCCCCCCCCCCCCCCC)CC2=C(Cl)C=CC=C2Cl.[I-]
• Target: AMPK
• Solubility: DMSO:131.25 mg/mL (221.16 mM)

Bioactivity

• In Vivo:
  Aldometanib, administered orally at dosages ranging from 0-10 mpk, effectively reduces blood glucose levels in lean mice and, when given at 2-10 mpk twice daily for a week, mitigates blood glucose and ameliorates fatty liver in obese hyperglycemic mice. Additionally, it addresses fatty liver and nonalcoholic steatohepatitis issues, and a regimen of 2 mpk twice daily over a month alleviates liver fibrosis in NASH mice. Moreover, Aldometanib extends the lifespan of C. elegans through the lysosomal pathway when administered orally at 0-50 μM for up to 50 days. In lean mice, dosages of 0-10 mpk lower fasting blood glucose, enhance glucose tolerance, and promote muscular TBC1D1 phosphorylation for glucose uptake. In obese hyperglycemic mice, a week-long administration of 2-10 mpk effectively lowers blood glucose, decreases hepatic TAG, and enhances insulin sensitivity through muscular AMPK dependencies, also diminishing fat mass. For NASH mice, a month-long administration of 2 mpk results in the reduction of NASH diagnostic histological scores, decreased hepatic cell apoptosis, reduced inflammatory liver responses, and improved glucose tolerance. In C. elegans, dosages of 0-50 μM improve oxidative stress resistance and bolster mitochondrial functions, while for C57BL/6 mice, administering 100 μg/mL orally rejuvenates muscle function and extends lifespan by increasing NAD+ levels and mitochondrial oxidative respiration.
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• In Vitro:
  Aldometanib (0-1000 nM; 2 h) activates AMPK through preventing aldolase from binding to FBP to engender a pseudo-starvation signal . Western Blot Analysis 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 Cell Line: MEFs cells Concentration: 5 nM Incubation Time: 2 h Result: Inhibited TRPVs and induces AXIN lysosomal translocation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Compound IA-47, Compound IA-47 (Br- base 2246625-81-8), CompoundIA47, Br- base 2246625-81-8, aldolase, Aldometanib

Compound Identifiers

PubChem CID

165413044