| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
angiotensin II receptor
Azilsartan mepixetil is a prodrug of azilsartan, which targets the angiotensin II type 1 (AT1) receptor. It acts as an antagonist of the angiotensin II receptor. By blocking the AT1 receptor, it prevents the vasoconstrictive and aldosterone-releasing effects of angiotensin II, leading to vasodilation and reduced blood pressure. |
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| ln Vitro |
In vitro, azilsartan mepixetil is a prodrug that is converted to its active form, azilsartan. Azilsartan demonstrates high potency and prolonged receptor binding at the AT1 receptor. It exhibits effective 24-hour blood pressure control in pharmacological models. The compound shows high affinity for the angiotensin II receptor and effective antagonism of angiotensin II-mediated effects.
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| ln Vivo |
In vivo, azilsartan mepixetil demonstrates stronger and longer-lasting blood pressure-lowering effects. It produces a more pronounced and prolonged effect on lowering heart rate. It has a higher level of safety compared to other agents. It is being studied for its potential benefits in heart failure, kidney protection, and metabolic syndrome.
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| Enzyme Assay |
In vitro receptor binding assays for azilsartan mepixetil typically involve competitive radioligand binding using membrane preparations expressing human AT1 receptors. Membranes are incubated with radiolabeled ligands and varying concentrations of the compound. IC50 values are calculated from displacement curves. Functional activity is assessed by measuring downstream signaling such as calcium mobilization or cAMP accumulation.
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| Cell Assay |
Cell-based assays for azilsartan mepixetil involve culturing cells expressing recombinant AT1 receptors (e.g., CHO or HEK-293 cells). Cells are treated with the compound at concentrations ranging from 0.1 nM to 10 µM. Receptor activation is measured by downstream signaling readouts. The prodrug conversion to azilsartan may be evaluated in cell-based systems. Cytotoxicity is assessed by standard viability assays.
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| Animal Protocol |
In vivo animal experiments for azilsartan mepixetil typically involve administration to hypertensive rodent models via oral gavage. Blood pressure is measured using telemetry or tail-cuff methods. Heart rate is monitored. Renal function and cardioprotective effects are evaluated by measuring biomarkers and histopathology. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues.
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| ADME/Pharmacokinetics |
Azilsartan mepixetil (molecular weight 678.69, formula C36H34N6O8) is a prodrug of azilsartan. It is orally active and has good bioavailability. It is metabolized to azilsartan, which has a long half-life supporting once-daily dosing. Detailed pharmacokinetic parameters are available in clinical pharmacology literature. It demonstrates effective 24-hour blood pressure control.
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| Toxicity/Toxicokinetics |
Azilsartan mepixetil has a higher level of safety compared to other agents. Common side effects may include dizziness, headache, and hyperkalemia. It is contraindicated in pregnancy. Comprehensive toxicological evaluation has been conducted in preclinical and clinical studies. The compound is generally well-tolerated in clinical settings.
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| References | |
| Additional Infomation |
Azilsartan mepixetil (CAS#: 1596357-16-2) is a prodrug of azilsartan and an angiotensin II type 1 (AT1) receptor antagonist. It has antihypertensive, renal, and cardioprotective effects. It demonstrates stronger, more prolonged blood pressure lowering and heart rate reduction with high safety. Molecular weight: 678.69, formula: C36H34N6O8.
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| Molecular Formula |
C36H34N6O8
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|---|---|
| Molecular Weight |
678.690568447113
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| Exact Mass |
678.24
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| Elemental Analysis |
C, 63.71; H, 5.05; N, 12.38; O, 18.86
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| CAS # |
1596357-16-2
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| Related CAS # |
Azilsartan mepixetil potassium; 2153458-32-1
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| PubChem CID |
137091385
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| Appearance |
White to off-white solid powder
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
50
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| Complexity |
1220
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JXSDNNVNQNYJSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H34N6O8/c1-6-46-34-39-29-13-9-12-28(33(43)48-23(5)49-36(45)47-19-30-22(4)37-20(2)21(3)38-30)31(29)42(34)18-24-14-16-25(17-15-24)26-10-7-8-11-27(26)32-40-35(44)50-41-32/h7-17,23H,6,18-19H2,1-5H3,(H,40,41,44)
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| Chemical Name |
1-[(3,5,6-trimethylpyrazin-2-yl)methoxycarbonyloxy]ethyl 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
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| Synonyms |
Azilsartan mepixetil
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~200 mg/mL (~294.7 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4734 mL | 7.3671 mL | 14.7343 mL | |
| 5 mM | 0.2947 mL | 1.4734 mL | 2.9469 mL | |
| 10 mM | 0.1473 mL | 0.7367 mL | 1.4734 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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