| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
AT1 Receptor (IC50 = 2.6 nM )
Azilsartan medoxomil monopotassium targets the angiotensin II receptor type 1 (AT1). It is a potent antagonist with an IC50 of 0.62 nM. By blocking the AT1 receptor, it prevents the binding of angiotensin II, a potent vasoconstrictor, thereby inhibiting the renin-angiotensin-aldosterone system (RAAS). This leads to vasodilation, reduced aldosterone secretion, and ultimately, a decrease in blood pressure. |
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| ln Vitro |
In vitro, in aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors. This suggests that azilsartan may have AT1-independent effects, which could contribute to its unique pharmacological profile.
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| ln Vivo |
In vivo, oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. Over a 24-week treatment period, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily.
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| Enzyme Assay |
For cell-free assays, the binding affinity of azilsartan to the AT1 receptor can be measured using radioligand binding assays. Membrane preparations from cells expressing the AT1 receptor are incubated with a radiolabeled ligand specific for the AT1 receptor and varying concentrations of azilsartan or its active metabolite. The IC50 value, representing the concentration required to inhibit 50% of the specific binding, is calculated from a competition binding curve.
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| Cell Assay |
For in vitro cellular assays, the antagonistic activity of azilsartan at the AT1 receptor can be assessed in cells expressing the receptor. Cells are treated with azilsartan and stimulated with angiotensin II. The inhibition of angiotensin II-induced responses, such as calcium mobilization or downstream signaling (e.g., ERK phosphorylation), is measured. The IC50 for receptor antagonism is calculated from dose-response curves.
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| Animal Protocol |
For in vivo studies, azilsartan medoxomil monopotassium is typically administered orally in animal models of hypertension, such as spontaneously hypertensive rats (SHR) or angiotensin II-infused models. Blood pressure is measured at various time points using telemetry or tail-cuff methods. Its efficacy is determined by comparing the blood pressure reduction in treated animals to that in a control group. Pharmacokinetic parameters are estimated from plasma samples analyzed by LC-MS/MS.
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| ADME/Pharmacokinetics |
Azilsartan medoxomil monopotassium (CAS 863031-24-7) has a molecular formula of C30H23KN4O8 and a molecular weight of 606.62 g/mol. Purity is >98% (HPLC). Solubility: 10 mM in DMSO. Storage: -20°C. It is a prodrug that is converted to the active moiety azilsartan. The compound is a potassium salt, which may influence its solubility and stability compared to the free acid form.
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| Toxicity/Toxicokinetics |
Azilsartan medoxomil monopotassium has a well-established clinical safety profile. Common side effects include diarrhea, nausea, and hypotension. It is generally well-tolerated. Serious side effects include angioedema and renal impairment. It is contraindicated during pregnancy. Its safety in patients with hepatic or renal impairment has been established through clinical studies.
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| References |
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| Additional Infomation |
Azilsartan potassium salt is an organopotassium salt, the monopotassium salt of azilsartan ester. It is a prodrug of azilsartan used to treat hypertension. It has the effects of a prodrug, an antihypertensive drug, and an angiotensin receptor antagonist. It contains azilsartan ester (1-).
See also: Azilsartan (with active moiety); Azilsartan potassium salt; Chlorthalidone (component). Azilsartan medoxomil monopotassium is an FDA-approved prescription drug for the treatment of hypertension. It is marketed under the brand name Edarbi. Its mechanism of action involves antagonism of the AT1 receptor. It is a prodrug that is hydrolyzed to the active moiety, azilsartan. It is available in oral tablet formulations. Its unique antiproliferative effects may contribute to its efficacy beyond blood pressure lowering. |
| Molecular Formula |
C₃₀H₂₃KN₄O₈
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|---|---|
| Molecular Weight |
606.62
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| Exact Mass |
606.12
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| Elemental Analysis |
C, 59.40; H, 3.82; K, 6.45; N, 9.24; O, 21.10
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| CAS # |
863031-24-7
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| Related CAS # |
Azilsartan medoxomil; 863031-21-4; Azilsartan; 147403-03-0; Azilsartan-d5; 1346599-45-8
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| PubChem CID |
23699544
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| Appearance |
White to off-white solid powder
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| LogP |
4.705
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
43
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[K].O=C1OC(COC(C2C3=C(N=C(N3CC3C=CC(C4C(C5NC(=O)ON=5)=CC=CC=4)=CC=3)OCC)C=CC=2)=O)=C(C)O1
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| InChi Key |
IHWFKDWIUSZLCJ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C30H24N4O8.K/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26;/h4-14H,3,15-16H2,1-2H3,(H,32,33,36);/q;+1/p-1
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| Chemical Name |
potassium;(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-1-oxa-2-aza-4-azanidacyclopent-2-en-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
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| Synonyms |
TAK-491 monopotassium; Azilsartan kamedoxomil; TAK491 monopotassium
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 114~125 mg/mL (200.5~219.9 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 | 1.6485 mL | 8.2424 mL | 16.4848 mL | |
| 5 mM | 0.3297 mL | 1.6485 mL | 3.2970 mL | |
| 10 mM | 0.1648 mL | 0.8242 mL | 1.6485 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05107960 | Recruiting | Drug: Azilsartan (TAK-536) | Hypertension | Takeda | December 16, 2021 | N/A |
| NCT05753696 | Recruiting | Drug: Azilsartan Drug: Losartan |
Proteinuria Blood Pressure |
Second Affiliated Hospital, School of Medicine, Zhejiang University |
April 1, 2023 | Not Applicable |
| NCT05947448 | Not yet recruiting | Drug: Azilsartan Medoxomil Potassium Tablet Drug: Levoamlodipine Maleate Table |
Essential Hypertension | Hasten Biopharmaceutical Co., Ltd. | January 1, 2024 | N/A |
| NCT02541669 | Completed | Drug: TAK-491 Drug: TAK-491 placebo |
Healthy Volunteer | Takeda | November 20, 2015 | Phase 1 |
| NCT02451150 | Completed | Drug: Azilsartan | Pediatric Hypertension | Takeda | August 2015 | Phase 3 |
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