Lixumistat acetate
Based on 1 publication(s) in Google Scholar
Lixumistat (IM156) acetate is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat acetate strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat acetate exhibits significant therapeutic effects on cognitive decline associated with brain aging and pulmonary fibrosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.88%
- CAS 番号: 1422365-94-3
- 分子式: C15H20F3N5O3
- 分子量:375.35
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Lixumistat acetate
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生物活性
製品説明
IC50 & Target
体外実験
Lixumistat (15 μM; 26 h) acetate 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) acetate 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) acetate potently and rapidly induces the phosphorylation of AMPK at the Thr172 site in NIH3T3 mouse fibroblasts[3].
Lixumistat (10 μM; 0-4 h) acetate 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.
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Cell Line:NIH3T3 cells
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Concentration:0.31, 0.62, 1.25, 2.5, 5, 10 μM (dose-response); 10 μM (time-course)
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Incubation Time:4 h (dose-response); 2, 4, 8 h (time-course)
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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.
体内実験
Lixumistat (10-30 mg/kg; i.g.; once daily for 14 consecutive days) acetate 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.
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Animal Model:C57BL/6J (male and female, 20~22 months of age)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 2 months
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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
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Animal Model:C57BL/6 (male, 6-7 weeks of age, bleomycin-induced pulmonary fibrosis)[2]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.g.; daily; 14 days
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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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1422365-94-3
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性状 Solid
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分子量 375.35
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分子式 C15H20F3N5O3
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Color White to off-white
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SMILES
N=C(N1CCCC1)NC(NC2=CC=C(OC(F)(F)F)C=C2)=N.CC(O)=O
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別名
IM156; HL156A; HL271 acetate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (133.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.66 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.66 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
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 and light). 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 | 2.6642 mL | 13.3209 mL | 26.6418 mL | 66.6045 mL |
| 5 mM | 0.5328 mL | 2.6642 mL | 5.3284 mL | 13.3209 mL | |
| 10 mM | 0.2664 mL | 1.3321 mL | 2.6642 mL | 6.6605 mL | |
| 15 mM | 0.1776 mL | 0.8881 mL | 1.7761 mL | 4.4403 mL | |
| 20 mM | 0.1332 mL | 0.6660 mL | 1.3321 mL | 3.3302 mL | |
| 25 mM | 0.1066 mL | 0.5328 mL | 1.0657 mL | 2.6642 mL | |
| 30 mM | 0.0888 mL | 0.4440 mL | 0.8881 mL | 2.2202 mL | |
| 40 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6651 mL | |
| 50 mM | 0.0533 mL | 0.2664 mL | 0.5328 mL | 1.3321 mL | |
| 60 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1101 mL | |
| 80 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8326 mL | |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6660 mL |
Lixumistat acetate 関連分類
HY-136093A 関連分類
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