1. GPCR/G Protein
  2. Angiotensin Receptor

Azilsartan medoxomil (Synonyms: TAK-491)

Cat. No.: HY-14736
Handling Instructions

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.

For research use only. We do not sell to patients.

Azilsartan medoxomil Chemical Structure

Azilsartan medoxomil Chemical Structure

CAS No. : 863031-21-4

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  • References

Description

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM [2] Target: AT1 receptor in vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors[1]. in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively [2]. Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan[3]. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide [4]. Clinical trial: Effect of Azilsartan on Aldosterone in Post-menopausal Females . Phase not specified

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7589 mL 8.7946 mL 17.5892 mL
5 mM 0.3518 mL 1.7589 mL 3.5178 mL
10 mM 0.1759 mL 0.8795 mL 1.7589 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

568.53

Formula

C₃₀H₂₄N₄O₈

CAS No.

863031-21-4

SMILES

O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C5=NC(ON5)=O)C=C3)=CC=C1)OCC6=C(C)OC(O6)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Azilsartan medoxomil
Cat. No.:
HY-14736
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Azilsartan medoxomil

Cat. No.: HY-14736