Aldometanib (LXY-05-029) is an aldolase inhibitor. Aldometanib activates lysosomal adenosine-phosphate-activated protein kinase AMPK and lowers blood glucose. Aldometanib may be utilized to study metabolic homeostasis.

Physicochemical Properties

Molecular Formula	C27H43CL2IN2
Molecular Weight	593.454198122025
Exact Mass	592.184
CAS #	2904601-67-6
PubChem CID	165413044
Appearance	Off-white to light yellow solid powder
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	1
Rotatable Bond Count	17
Heavy Atom Count	32
Complexity	424
Defined Atom Stereocenter Count	0
InChi Key	QGSVKLIYXRLMTB-UHFFFAOYSA-M
InChi Code	InChI=1S/C27H43Cl2N2.HI/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-20-30-21-22-31(24(30)2)23-25-26(28)18-17-19-27(25)29;/h17-19,21-22H,3-16,20,23H2,1-2H3;1H/q+1;/p-1
Chemical Name	1-[(2,6-dichlorophenyl)methyl]-3-hexadecyl-2-methylimidazol-1-ium;iodide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In order to produce a pseudo-starvation signal, aldolase cannot bind to FBP, which is how aldometanib (0-1000 nM; 2 hours) activates AMPK [1].
ln Vivo	In thin mice, aldometanib (oral; 0–10 mpk) lowers blood glucose levels [1]. In obese hyperglycemic rats, aldometanib (oral; 2–10 mpk; twice daily; for a week) reduces blood sugar and ameliorates fatty liver disease [1]. Non-alcoholic steatohepatitis and fatty liver disease are reduced by aldometanib [1]. In NASH mice, aldometanib (oral; 2mpk; twice-daily; for one month) decreases liver fibrosis [1]. C may live longer if administered oral (0–50 μM; 0–50 days) aldometanib. elegans by means of the lysosomal route [1].
Cell Assay	Western Blot Analysis[1] Cell Types: Mouse primary hepatocytes, MEFs cells Tested Concentrations: 0-1000 nM Incubation Duration: 2 h Experimental Results: Activated AMPK in mouse embryonic fibroblasts (MEFs) and mouse primary hepatocytes cells. Immunofluorescence[1] Cell Types: MEFs cells Tested Concentrations: 5 nM Incubation Duration: 2 h Experimental Results: Inhibited TRPVs and induces AXIN lysosomal translocation.
Animal Protocol	Animal/Disease Models: Lean mice[1] Doses: 0-10 mpk Route of Administration: Oral Experimental Results: diminished fasting blood glucose and improved glucose tolerance, promoted muscular TBC1D1 phosphorylation and glucose uptake. Animal/Disease Models: Obese hyperglycaemic mice[1] Doses: 2-10 mpk Route of Administration: po (oral gavage) twice (two times) daily, for a week Experimental Results: diminished blood glucose, lowered blood glucose in a muscular AMPK-dependent manner diminished hepatic TAG, improved insulin sensitivity, increased glucose disposal rates, inhibited TAG synthesis in liver and primary hepatocytes, diminished fat mass. Animal/Disease Models: NASH mice[1] Doses: 2 mpk Route of Administration: po (oral gavage) twice-daily, for a month Experimental Results: diminished histological scores used to describe the features of NASH, diminished apoptosis rate of hepatic cells, inhibited inflammatory responses in the liver of NASH mice and improved glucose tolerance of NASH mice. Animal/Disease Models: C. elegans[1] Doses: 0-50 μM Route of Administration: po (oral gavage) 0 -50 days Experimental Results: Promoted oxidative stress resistance and mitoch
References	[1]. The aldolase inhibitor aldometanib mimics glucose starvation to activate lysosomal AMPK. Nat Metab. 2022 Oct 10.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (168.51 mM)

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.