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

Lixumistat hydrochloride  (Synonyms: HL271; IM156 hydrochloride; HL156A hydrochloride)

Cat. No.: HY-136093 Purity: 99.25%
Handling Instructions Technical Support

Lixumistat (IM156) hydrochloride is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat hydrochloride strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat hydrochloride 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 hydrochloride

Lixumistat hydrochloride Chemical Structure

CAS No. : 1422365-52-3

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

Based on 1 publication(s) in Google Scholar

Other Forms of Lixumistat hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lixumistat hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

AMPK[1][2], OXPHOS[3]

In Vitro

Lixumistat (15 μM; 26 h) hydrochloride 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) hydrochloride 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) hydrochloride potently and rapidly induces the phosphorylation of AMPK at the Thr172 site in NIH3T3 mouse fibroblasts[3].
Lixumistat (10 μM; 0-4 h) hydrochloride 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 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.
In Vivo

Lixumistat (50 mg/kg; p.o.; administered daily for 2 months) hydrochloride 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) hydrochloride 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

351.76

Formula

C13H17ClF3N5O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(N1CCCC1)NC(NC2=CC=C(OC(F)(F)F)C=C2)=N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (118.46 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 2.8428 mL 14.2142 mL 28.4285 mL
5 mM 0.5686 mL 2.8428 mL 5.6857 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.25%

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 (sealed storage, away from moisture). 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 2.8428 mL 14.2142 mL 28.4285 mL 71.0712 mL
5 mM 0.5686 mL 2.8428 mL 5.6857 mL 14.2142 mL
10 mM 0.2843 mL 1.4214 mL 2.8428 mL 7.1071 mL
15 mM 0.1895 mL 0.9476 mL 1.8952 mL 4.7381 mL
20 mM 0.1421 mL 0.7107 mL 1.4214 mL 3.5536 mL
25 mM 0.1137 mL 0.5686 mL 1.1371 mL 2.8428 mL
30 mM 0.0948 mL 0.4738 mL 0.9476 mL 2.3690 mL
40 mM 0.0711 mL 0.3554 mL 0.7107 mL 1.7768 mL
50 mM 0.0569 mL 0.2843 mL 0.5686 mL 1.4214 mL
60 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1845 mL
80 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8884 mL
100 mM 0.0284 mL 0.1421 mL 0.2843 mL 0.7107 mL
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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.

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Product Name:
Lixumistat hydrochloride
Cat. No.:
HY-136093
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