Azilsartan (medoxomil monopotassium)
Based on 2 publication(s) in Google Scholar
Azilsartan medoxomil (TAK 491) monopotassium, a prodrug form of Azilsartan (HY-14914), is an orally active angiotensin II receptor type 1 antagonist. Azilsartan medoxomil monopotassium can be used for the study of essential hypertension.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.00%
- CAS. Nr.: 863031-24-7
- Formel: C30H23KN4O8
- Molecular Weight:606.62
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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AzilsartanAT1 Antagonist -
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IrbesartanAT1 Receptor Blocker -
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Publications Citing Use of MedChemExpress (MCE) Azilsartan (medoxomil monopotassium)
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Biologische Aktivität
Beschreibung
IC50 & Target
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AT1 Receptor |
In Vivo
Azilsartan medoxomil (0.1-10 mg/kg in peanut butter, once daily) monopotassium inhibits vascular wall expression of plasminogen activator inhibitor type-I (PAI-1) protein, and potentially facilitates the stabilization of atherosclerotic plaques in ApoE knockout mice on a high fat diet rendered overexpressors of PAI-1 in VSMCs[5].
Azilsartan medoxomil (0.03-10 mg/kg, oral gavage, once a day) monopotassium reduces myocardial infarct size in rats[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[6]
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Dosage:0.03-10 mg/kg
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Administration:oral gavage, once a day for 4 days
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Result:Reduced myocardial infarct size.
Increased calcium-dependent nitric oxide synthase activity.
Increased Akt, ERK 1/2 and eNOS phosphorylation and inhibited BAX activation.
Chemical Information
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CAS. Nr. 863031-24-7
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Appearance Solid
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Molecular Weight 606.62
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Formel C30H23KN4O8
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Color White to off-white
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SMILES
O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C5=NC(O[N-]5)=O)C=C3)=CC=C1)OCC6=C(C)OC(O6)=O.[K+]
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Synonyms
Azilsartan kamedoxomil; TAK 491 monopotassium
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Int Immunopharmacol
Repurposing Azilsartan medoxomil attenuates periodontitis by targeting SERPINB9 to promote apoptosis of IL1B+ macrophages. [Abstract]2026 May 15:177:116523. PMID: 41864017
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 175 mg/mL (288.48 mM; Need ultrasonic; 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
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)
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.
Protokoll
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Kajiya T, Ho C, Wang J, Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83. [Content Brief]
[2]. Kusumoto K, Igata H, Ojima M, Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models. [Content Brief]
[3]. Perry CM. Azilsartan medoxomil: a review of its use in hypertension. Clin Drug Investig. 2012 Sep 1;32(9):621-39. [Content Brief]
[4]. Pierini D, Anderson KV. Azilsartan medoxomil/chlorthalidone: a new fixed-dose combination antihypertensive. Ann Pharmacother. 2013 May;47(5):694-703. [Content Brief]
[5]. French CJ, et al. The angiotensin receptor blocker, azilsartan medoxomil (TAK-491), suppresses vascular wall expression of plasminogen activator inhibitor type-I protein potentially facilitating the stabilization of atherosclerotic plaques. J Cardiovasc Pharmacol. 2011 Aug;58(2):143-8. [Content Brief]
[6]. Ye Y, et al. Additive effect of TAK-491, a new angiotensin receptor blocker, and pioglitazone, in reducing myocardial infarct size. Cardiovasc Drugs Ther. 2010 Apr;24(2):107-20. [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). 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 |
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| DMSO | 1 mM | 1.6485 mL | 8.2424 mL | 16.4848 mL | 41.2120 mL |
| 5 mM | 0.3297 mL | 1.6485 mL | 3.2970 mL | 8.2424 mL | |
| 10 mM | 0.1648 mL | 0.8242 mL | 1.6485 mL | 4.1212 mL | |
| 15 mM | 0.1099 mL | 0.5495 mL | 1.0990 mL | 2.7475 mL | |
| 20 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0606 mL | |
| 25 mM | 0.0659 mL | 0.3297 mL | 0.6594 mL | 1.6485 mL | |
| 30 mM | 0.0549 mL | 0.2747 mL | 0.5495 mL | 1.3737 mL | |
| 40 mM | 0.0412 mL | 0.2061 mL | 0.4121 mL | 1.0303 mL | |
| 50 mM | 0.0330 mL | 0.1648 mL | 0.3297 mL | 0.8242 mL | |
| 60 mM | 0.0275 mL | 0.1374 mL | 0.2747 mL | 0.6869 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5151 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1648 mL | 0.4121 mL |
Azilsartan (medoxomil monopotassium) Related Classifications
HY-17458 Related Classifications
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