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Tocris/Azilsartan/4553/50/50 mg

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货号: 4553/50

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

Keywords: Azilsartan, supplier, angiotensin, II, receptor, inverse, agonist, inhibits, inhibitors, antihypertensive, antiproliferative, PAI-1, expression, plasminogen, activator, inhibitor, 1, potent, selective, slow, dissociating, Angiotensin, AT1, Receptors, Angiotensin, AT1, Receptors, Tocris Bioscience

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