2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  3. Mitochondrial Metabolism AMPK
  4. Lixumistat

Lixumistat  (Synonyms: IM156 free base; HL156A free base; HL271 free base)

Cat. No.: HY-136093B Purity: 99.33%
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Lixumistat (IM156 free base) is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat exhibits significant therapeutic effects on cognitive decline associated with brain aging and pulmonary fibrosis.

For research use only. We do not sell to patients.

Lixumistat

Lixumistat Chemical Structure

CAS No. : 1422365-93-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
25 mg In-stock
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100 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lixumistat:

Lixumistat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lixumistat

View All AMPK Isoform Specific Products:

View All Isoforms
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lixumistat (IM156 free base) is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat exhibits significant therapeutic effects on cognitive decline associated with brain aging and pulmonary fibrosis[1][2][3].

In Vitro

Lixumistat (15 μM; 26 h) potently inhibits TGFβ1-induced mitochondrial oxidative phosphorylation reprogramming in WI-38 human embryonic lung fibroblasts, with an IC50 of 14.7 μM, and does not alter TGFβ1-induced glycolytic changes[2].
Lixumistat (7.5-30 μM; 26-48 h) inhibits TGFβ1-induced myofibroblast differentiation (α-SMA expression, IC50 = 21.3 μM) and collagen deposition (IC50 = 13.2 μM) in a dose-dependent manner in WI-38 human embryonic lung fibroblasts without reducing cell viability[2].
Lixumistat (0.31-10 μM; 2-8 h) potently and rapidly induces the phosphorylation of AMPK at the Thr172 site in NIH3T3 mouse fibroblasts[3].
Lixumistat (10 μM; 0-4 h) promotes the proteasome-dependent degradation of PER2 and CRY1 proteins in NIH3T3 mouse fibroblasts when co-incubated with Cycloheximide (HY-12320)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lixumistat Related Antibodies

Western Blot Analysis[3]

Cell Line: NIH3T3 mouse fibroblast cells
Concentration: 0.31, 0.62, 1.25, 2.5, 5, 10 μM (dose-response); 10 μM (time-course)
Incubation Time: 4 h (dose-response); 2, 4, 8 h (time-course)
Result: Dose-dependently stimulated AMPK phosphorylation, with significant increases observed at concentrations ≥ 1.25 μM after 4 h incubation.
Increased AMPK phosphorylation in a time-dependent manner, with significant elevations detected as early as 2 h after treatment with 10 μM.

Western Blot Analysis[3]

Cell Line: NIH3T3 mouse fibroblast cells
Concentration: 10 μM (with 30 μg/mL CHX); 10 μM (with 30 μg/mL CHX + 50 μM MG132)
Incubation Time: 0, 1, 2, 4 h (with 30 μg/mL CHX); 0, 1, 2, 4 h (with 30 μg/mL CHX + 50 μM MG132)
Result: Enhanced the degradation of V5-tagged PER2 and FLAG-tagged CRY1 proteins in the presence of CHX, with protein levels decreasing more rapidly than in control cells.
Completely blocked this enhanced degradation when co-treated with MG132.
In Vivo

Lixumistat (50 mg/kg; p.o.; administered daily for 2 months) significantly ameliorates age-related cognitive decline in aged C57BL/6J mice[1].
Lixumistat (10-30 mg/kg; i.g.; once daily for 14 consecutive days) dose-dependently alleviates pulmonary fibrosis and inflammatory responses in male C57BL/6 mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male and female, 20~22 months of age)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 2 months
Result: Significantly improved age-related cognitive decline in aged C57BL/6J mice, with a 23.2% increase in novel object recognition discrimination ratio, 27.4% increase in spatial working memory %SAP, 47.3% increase in contextual fear memory freezing level, and 91.6% increase in hippocampal pAMPK relative intensity compared to controls
Animal Model: C57BL/6 (male, 6-7 weeks of age, bleomycin-induced pulmonary fibrosis)[2]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.g.; daily; 14 days
Result: Attenuated body weight loss, with significant improvements observed on study days 19 and 21.
Reduced bleomycin-induced increases in lung weight at both doses, with greater efficacy at 30 mg/kg.
Significantly reduced modified Ashcroft fibrosis scores.
Molecular Weight

315.29

Formula

C13H16F3N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(N1CCCC1)NC(NC2=CC=C(OC(F)(F)F)C=C2)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (317.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1717 mL 15.8584 mL 31.7168 mL
5 mM 0.6343 mL 3.1717 mL 6.3434 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1717 mL 15.8584 mL 31.7168 mL 79.2921 mL
5 mM 0.6343 mL 3.1717 mL 6.3434 mL 15.8584 mL
10 mM 0.3172 mL 1.5858 mL 3.1717 mL 7.9292 mL
15 mM 0.2114 mL 1.0572 mL 2.1145 mL 5.2861 mL
20 mM 0.1586 mL 0.7929 mL 1.5858 mL 3.9646 mL
25 mM 0.1269 mL 0.6343 mL 1.2687 mL 3.1717 mL
30 mM 0.1057 mL 0.5286 mL 1.0572 mL 2.6431 mL
40 mM 0.0793 mL 0.3965 mL 0.7929 mL 1.9823 mL
50 mM 0.0634 mL 0.3172 mL 0.6343 mL 1.5858 mL
60 mM 0.0529 mL 0.2643 mL 0.5286 mL 1.3215 mL
80 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9912 mL
100 mM 0.0317 mL 0.1586 mL 0.3172 mL 0.7929 mL
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Lixumistat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lixumistat1422365-93-2IM156HL156AHL271IM 156IM-156HL 271HL-271Mitochondrial MetabolismAMPKAMP-activated protein kinasemitochondrial complex 1MCF7 human breast cancer cellsPER2human pulmonary fibroblastsmicehippocampusWI-38 human embryonic lung fibroblastsCRY1NIH3T3 mouse fibroblast cellsInhibitorinhibitorinhibit

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