Azilsartan medoxomil
Based on 2 publication(s) in Google Scholar
Azilsartan medoxomil (TAK 491), a prodrug form of Azilsartan (HY-14914), is an orally active angiotensin II receptor type 1 antagonist. Azilsartan medoxomil can be used for the study of essential hypertension.
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- Pureza : 99.07%
- No. CAS: 863031-21-4
- Fòrmula: C30H24N4O8
- Peso molecular:568.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-14914
AzilsartanAT1 Antagonist -
HY-17004
OlmesartanAT1R Antagonist -
HY-17005
Olmesartan medoxomil -
HY-15531
VenetoclaxBCL-2 Inhibitor -
HY-10984
PomalidomideImmunomodulatory Agent -
HY-17512
LosartanAngiotensin II Receptor Antagonist -
HY-B0202
IrbesartanAT1 Receptor Blocker -
HY-18204
ValsartanAngiotensin II Receptor Antagonist -
HY-B0205
CandesartanAngiotensin II AT1-Receptor Blocker -
HY-13955
TelmisartanAngiotensin II Type 1 Receptor -
HY-18204A
Sacubitril/ValsartanARN Inhibitor -
HY-B0195
TranilastAnti-allergic Agent
Publications Citing Use of MedChemExpress (MCE) Azilsartan medoxomil
MoreVer todos los productos específicos de isoformas Angiotensin Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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AT1 Receptor |
In Vivo
Azilsartan medoxomil (0.1-10 mg/kg in peanut butter, once daily) 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) 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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 863031-21-4
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Appearance Solid
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Peso molecular 568.53
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Fòrmula C30H24N4O8
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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(ON5)=O)C=C3)=CC=C1)OCC6=C(C)OC(O6)=O
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Synonyms
TAK-491
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (219.87 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (3.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7589 mL | 8.7946 mL | 17.5892 mL | 43.9731 mL |
| 5 mM | 0.3518 mL | 1.7589 mL | 3.5178 mL | 8.7946 mL | |
| 10 mM | 0.1759 mL | 0.8795 mL | 1.7589 mL | 4.3973 mL | |
| 15 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9315 mL | |
| 20 mM | 0.0879 mL | 0.4397 mL | 0.8795 mL | 2.1987 mL | |
| 25 mM | 0.0704 mL | 0.3518 mL | 0.7036 mL | 1.7589 mL | |
| 30 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL | |
| 40 mM | 0.0440 mL | 0.2199 mL | 0.4397 mL | 1.0993 mL | |
| 50 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 mL | |
| 60 mM | 0.0293 mL | 0.1466 mL | 0.2932 mL | 0.7329 mL | |
| 80 mM | 0.0220 mL | 0.1099 mL | 0.2199 mL | 0.5497 mL | |
| 100 mM | 0.0176 mL | 0.0879 mL | 0.1759 mL | 0.4397 mL |
Azilsartan medoxomil Related Classifications
HY-14736 Related Classifications
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