Azilsartan

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Cat.No. 4553 - Azilsartan | C25H20N4O5 | CAS No. 147403-03-0
Description: Potent AT1 receptor 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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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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Citations for Azilsartan

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Literature in this Area

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Pathways for Azilsartan

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