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Submit ReviewAzilsartan 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.
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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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.65 | 100 |
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 |
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
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