Cat. No.: HY-136093B

Lixumistat

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

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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.

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Pureté: 99.33%
CAS No.: 1422365-93-2
Formule: C₁₃H₁₆F₃N₅O
Masse moléculaire:315.29

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lixumistat Chemical Structure

CAS No.: 1422365-93-2

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform AMPK :

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.

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.

Chemical Information

CAS No. 1422365-93-2
Appearance Solid
Masse moléculaire 315.29
Formule C₁₃H₁₆F₃N₅O
Color White to off-white
SMILES

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

IM156 free base; HL156A free base; HL271 free base
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cell Death Discov

Long-term adaptation of lymphoma cell lines to hypoxia is mediated by diverse molecular mechanisms that are targetable with specific inhibitors. [Abstract]

2025 Feb 18;11(1):65. PMID: 39966387

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1717 mL

15.8584 mL

31.7168 mL

5 mM

0.6343 mL

3.1717 mL

6.3434 mL

10 mM

0.3172 mL

1.5858 mL

3.1717 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
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- Swedish - SV (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Bang E, et al. The Improving Effect of HL271, a Chemical Derivative of Metformin, a Popular Drug for Type II Diabetes Mellitus, on Aging-induced Cognitive Decline. Exp Neurobiol. 2018;27(1):45-56. [Content Brief]

[2]. Willette RN, et al. Modulation of Oxidative Phosphorylation with IM156 Attenuates Mitochondrial Metabolic Reprogramming and Inhibits Pulmonary Fibrosis. J Pharmacol Exp Ther. 2021;379(3):290-300. [Content Brief]

[3]. Row H, et al. HL271, a novel chemical compound derived from metformin, differs from metformin in its effects on the circadian clock and metabolism. Biochem Biophys Res Commun. 2016;469(3):783-789. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Lixumistat

1 Cited Publications

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Lixumistat

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Anti-Aging Compound Library

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Mitochondria-Targeted Compound Library

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Anti-Pulmonary Fibrosis Compound Library

Cuproptosis Compound Library

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Pain-Related Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

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Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Lixumistat

Voir tous les produits spécifiques à Isoform AMPK

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lixumistat Related Classifications

HY-136093B Related Classifications