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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Azilsartan (TAK-536; TAK536; Edarbi; Ipreziv) is a potent and orally bioavailable angiotensin II type 1 (AT1) receptor antagonist with antihypertensive effects. It inhibit the RAAS pathway with an IC50 of 2.6 nM and has been approved for use in the treatment of hypertension. Azilsartan was developed by Takeda Pharmaceuticals for the treatment of hypertension. Azilsartan lowers blood pressure by blocking the action of angiotensin II, a vasopressor hormone. Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors. Azilsartan also inhibits the accumulation of AII-induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM. Azilsartan medoxomil is a useful and attractive new option for lowering BP in patients with essential hypertension, particularly for those not able to tolerate other antihypertensive drugs.
| ln Vitro |
Azilsartan (0-200 μM, 0-72 hours) decreases HepG2 cell viability [5]. In HepG2 cells, azilartan (100 μM) causes apoptosis during a 24-hour period [5]. With an IC50 of 2.6 nM, acilestan prevents the particular binding of 125I-Sar1-Ile8-AII to the human angiotensin type 1 receptor[3]. Azilsartan efficiently suppresses aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation [5]. Compared to valsartan, azilartan has a larger influence on adipogenesis and the expression of genes encoding leptin, adiponectin, PPARδ, and peroxisome proliferator-activated receptor-alpha (PPARα). Influence [1].
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| ln Vivo |
In obese Koletsky rats, azilstaran (0–3 mg/kg) administered orally once daily for five days lowers systolic blood pressure (SBP) at a dose of 2 mg/kg[2]. Azilsartan (0–2 mg/kg, orally administered, once daily for 21 days) reduces basal plasma insulin levels and blood pressure[2]. Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) provides defense against secondary brain injury caused by ischemia[4].
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| Cell Assay |
Cell proliferation assay [5]
Cell Types: HepG2 and KDR Cell Tested Concentrations: 5, 25, 50, 100 and 200 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: The viability of HepG2 cells gradually diminished by increasing the incubation time and duration. At the same dose, the inhibitory concentration (IC 50%) of azilsartan on HepG2 cells at the 24-hour treatment time point was 100 μM, and under similar treatment conditions, no obvious cytotoxic effect was observed in KDR epithelial normal cells. Apoptosis analysis [5] Cell Types: HepG2 Cell Tested Concentrations: 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: 57.2% early and 0.52% late apoptosis were induced after 24 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: Male Wistar-Kyoto (WKY) rats, obese Koletsky rats (n=6 per group)[2]
Doses: 0, 1, 2 and 3 mg/kg Route of Administration: po (oral gavage), one time/day (9:00-10:00 hrs (hours)) for 5 days Experimental Results: diminished SBP (systolic blood pressure) in obese Koletsky rats to that of normal rats at 2 mg/kg, whereas the 3 mg/kg dose elicited hypotension. Animal/Disease Models: Obese Koletsky rats (16, n = 8 per group)[2] Doses: 0 and 2 mg/kg Route of Administration: po (oral gavage), one time/day (9:00-10:00 hrs (hours)) for 21 days Experimental Results: Lowered blood pressure, basal plasma insulin concentration and the homeostasis model assessment of insulin resistance index, and inhibited over-increase of plasma glucose and insulin concentrations during oral glucose tolerance test. Animal/Disease Models: Male Wistar Rats (240–280 g)[4] Doses: 0, 2, and 4 mg/kg Route of Administration: Orally, daily for 9 days, starting 7 days before the day of surgery Experimental Results: Individual treatments with Azilsartan (2 & 4 mg/kg) and Coenzyme Q10 (20 & 40 mg/kg) Dramatically attenuate |
| References |
[1]. Kajiya T, et al. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83.
[2]. Zhao M, et al. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats. Diabetes Obes Metab. 2011 Dec;13(12):1123-9. [3]. Ojima M, et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8. [4]. Gupta V, et al. Neuroprotective potential of azilsartan against cerebral ischemic injury: Possible involvement of mitochondrial mechanisms. Neurochem Int. 2020 Jan;132:104604. [5]. Ahmadian E, et al. Novel angiotensin receptor blocker, azilsartan induces oxidative stress and NFkB-mediated apoptosis in hepatocellular carcinoma cell line HepG2. Biomed Pharmacother. 2018 Mar;99:939-946. |
| Molecular Formula |
C25H20N4O5
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| Molecular Weight |
456.45
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| CAS # |
147403-03-0
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| Related CAS # |
Azilsartan medoxomil;863031-21-4;Azilsartan-d5;1346599-45-8;Azilsartan-d4;1794817-45-0;Azilsartan medoxomil monopotassium;863031-24-7
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| SMILES |
O(C([H])([H])C([H])([H])[H])C1=NC2=C([H])C([H])=C([H])C(C(=O)O[H])=C2N1C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])C1=C([H])C([H])=C([H])C([H])=C1C1=NOC(N1[H])=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol :30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1908 mL | 10.9541 mL | 21.9082 mL | |
| 5 mM | 0.4382 mL | 2.1908 mL | 4.3816 mL | |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1908 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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