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Submit ReviewAzilsartan
Description: Potent AT1 inverse agonist; antihypertensive
Chemical Name: 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid
Purity: ≥98% (HPLC)
Biological Activity for Azilsartan
Azilsartan is a 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 for Azilsartan
Azilsartan is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Azilsartan
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Azilsartan
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.65 | 100 |
Preparing Stock Solutions for Azilsartan
The following data is based on the product molecular weight 456.45. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for Azilsartan
References for Azilsartan
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Azilsartan, please let us know.
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Citations for Azilsartan
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Literature in this Area
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