Biological Activity
Potent angiotensin II type 1 (AT1) receptor inverse agonist (IC50 = 2.6 nM at the human AT1 receptor). Inhibits angiotensin II-induced IP1 accumulation in COS-7 cells; decreases maximal contraction of rabbit aortic strips in a concentration-dependent manner (pD'2 = 9.9). Antihypertensive; prevents vascular cell proliferation and expression of PAI-1.
Compound Libraries
Azilsartan is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 456.45 |
| Formula | C25H20N4O5 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 147403-03-0 |
| PubChem ID | 9825285 |
| InChI Key | KGSXMPPBFPAXLY-UHFFFAOYSA-N |
| Smiles | O=C1NC(C2=CC=CC=C2C(C=C5)=CC=C5CN4C3=C(C(O)=O)C=CC=C3N=C4OCC)=NO1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.65 | 100 | |
| ethanol | 4.56 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 456.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.19 mL | 10.95 mL | 21.91 mL |
| 5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.19 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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References
References are publications that support the products' biological activity.
Kajiya et al (2011) Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J.Hypertens. 29 2476 PMID: 21986624
French et al (2011) 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. 58 143 PMID: 21558880
Ojima et al (2011) In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J.Pharmacol.Exp.Ther. 336 801 PMID: 21123673
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