Azilsartan Medoxomil

Catalog No.S3057 Synonyms: TAK-491

Azilsartan Medoxomil Chemical Structure

Molecular Weight(MW): 568.53

Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.

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In DMSO USD 390 In stock
USD 170 In stock
USD 270 In stock
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  • (B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.

    Sci Rep, 2015, 5:8116.. Azilsartan Medoxomil purchased from Selleck.

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Biological Activity

Description Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.
Targets
AT1 receptor [1]
2.6 nM
In vitro

Azilsartan medoxomil is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone. [2] Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a >10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM). [1]

Protocol

Kinase Assay:[1]
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Radioligand Binding:

A radioligand binding assay is performed by using human AT1 receptor-coated microplates containing 4.4 to 6.2 fmol of receptors/well (10 μg of membrane protein/well). Membrane-coated wells are incubated with 45 μl of assay buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, and 0.005% CHAPS, pH 7.4) containing various concentrations of test compounds at room temperature. After 90 min, 5 μl of 125I-Sar1-Ile8-AII (final concentration 0.6 nM) dissolved in assay buffer is added to the wells, and the plate is incubated for 5 h. In each step, the plate is briefly and gently shaken on a plate shaker.
Cell Research:[1]
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  • Cell lines: COS-7
  • Concentrations: ~10 nM
  • Incubation Time: 2 h
  • Method: Measurement of Inositol 1-Phosphate Accumulation. Twentyfour hours after transfections with human AT1-expressing plasmids, the cells are starved by changing the culture medium to starvation buffer (1 mM CaCl2, 0.5 mM MgCl2, 4.2 mM KCl, 146 mM NaCl, 5.5 mM glucose, and 10 mM HEPES, pH 7.3). Then, 5 μl/well of the test compounds dissolved in starvation buffer is added to the cells at the indicated concentrations, and they are pretreated for the indicated times. Two hours after starvation, LiCl is added to a final concentration of 50 mM with or without angiotensin II 10 nM, and the cells are further incubated for the indicated times at 37°C. In washout experiments, the cells are washed once with 100 μl/well of starvation buffer to remove unbound compounds before stimulation with angiotensin II. The accumulation of inositol 1-phosphate (IP1) is measured by using a IP-One Tb kit. The fluorescence resonance energy transfer signal is measured on a plate reader.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 114 mg/mL (200.51 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 568.53
Formula

C30H24N4O8

CAS No. 863031-21-4
Storage powder
Synonyms TAK-491

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02756819 Recruiting Hypertension Takeda June 2016 Phase 4
NCT02541669 Recruiting Healthy Volunteer Takeda November 2015 Phase 1
NCT02480764 Recruiting Essential Hypertension Takeda September 2015 Phase 3
NCT02517866 Completed Essential Hypertension|Type 2 Diabetes Mellitus Takeda August 2015 Phase 4
NCT02235909 Recruiting Hypertension Arbor Pharmaceuticals, Inc. December 2014 Phase 3
NCT02203916 Completed Hypertension Takeda July 2014 Phase 3

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RAAS Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID