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    Azilsartan Medoxomil (TAK 491)
    Azilsartan Medoxomil (TAK 491)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1793
    CAS #: 863031-21-4 Purity ≥98%

    Description: Azilsartan Medoxomil (formerly also known as TAK-491), the ester prodrug of Azilsartan (TAK-536), is a potent and orally bioavailable angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM. It is used for the treatment of hypertension. Azilsartan lowers blood pressure by blocking the action of angiotensin II. Azilsartan also inhibits the accumulation of AII-induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM. Azilsartan medoxomil is a useful and attractive new option for lowering BP in patients with essential hypertension, particularly for those not able to tolerate other antihypertensive drugs.  

    References: J Pharmacol Exp Ther. 2011 Mar;336(3):801-8; Am J Hypertens. 2007 May;20(5):579-86.

    Related CAS#: 863031-24-7 (potassium); 1824707-75-6 (trimethylethanolamine); 147403-03-0 (free acid); 1346599-45-8 (Azilsartan D5);

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    Molecular Weight (MW)568.53
    FormulaC30H24N4O8 
    CAS No.863031-21-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 114 mg/mL (200.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
    InChi Key: QJFSABGVXDWMIW-UHFFFAOYSA-N
    InChi Code: InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)
    SMILES Code: 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
    SynonymsTAK-491; TAK 491; TAK491; Azilsartan medoxomil; Azilsartan medoxomil potassium; trade name: Edarbi. Ipreziv.


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    In Vitro

    In vitro activity: 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. 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).


    Kinase Assay: 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 Assay: 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.

    In VivoIn Koletsky rats, Azilsartan treatment lowers blood pressure, basal plasma insulin concentration and the homeostasis model assessment of insulin resistance index, and inhibited over-increase of plasma glucose and insulin concentrations during oral glucose tolerance test. Azilsartan downregulates 11β-hydroxysteroid dehydrogenase type 1 expression. 
    Animal modelMale Wistar-Kyoto (WKY) rats, obese Koletsky (fak/fak) rats 
    Formulation & DosageSuspended in 5% Gum Arabic; 1, 2, and 3 mg/kg; Oral gavage
    References

    J Pharmacol Exp Ther. 2011 Mar;336(3):801-8; Clin Ther. 2011 Nov;33(11):1577-89; J Pharmacol Exp Ther. 2011 Mar;336(3):801-8; Am J Hypertens. 2007 May;20(5):579-86; Diabetes Obes Metab. 2011 Dec;13(12):1123-9.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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