1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Azilsartan

Azilsartan (Synonyms: TAK-536)

Cat. No.: HY-14914 Purity: 99.09%
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Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM.

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

Azilsartan Chemical Structure

Azilsartan Chemical Structure

CAS No. : 147403-03-0

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
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100 mg USD 156 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Azilsartan:

Top Publications Citing Use of Products

    Azilsartan purchased from MCE. Usage Cited in: Oncotarget. 2017 Apr 11;8(15):24099-24109.

    Rats are orally administered with vehicle or Azilsartan (5 mg/kg/d) during the four-week rotenone (2.5 mg/kg/d) infusion. A. TH-immunoreactive neurons in the SN of each group. B. Quantitative analysis of TH-positive neurons in the SN of each group. Scale bar: 500 μm. C. The activity of caspase-3 in the SN is measured by a colorimetric assay kit.
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    Description

    Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM. IC50 Value: 2.6 nM [1] Target: AT1 receptor in vitro: Azilsartan inhibited the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50 of 2.6 nM. The inhibitory effect of AZL persisted after washout of the free compound (IC(50) value of 7.4 nM). AZL also inhibited the accumulation of AII-induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nmol; this effect was resistant to washout (IC50 value of 81.3 nM). Olmesartan and valsartan inhibited IP1 accumulation with IC50 values of 12.2 and 59.8 nM, respectively [1]. Azilsartan is not readily biodegradable. Results of the water sediment study demonstrated significant shifting of azilsartan metabolites to sediment. Based on the equilibrium partitioning method, metabolites are unlikely to pose a risk to sediment-dwelling organisms [2]. in vivo: 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 azilsartanmedoxomil/hydrochlorothiazide [3]. Both TAK-536 and candesartan suppressed the increase in plasma glucose level in the OGTT without significant change in insulin concentration and improved insulin sensitivity. In adipose tissue, TAK-536 and candesartan reduced TNF-alpha expression but increased the expression of adiponectin, PPARgamma, C/EBalpha, and aP2 [4]. Clinical trial: New Angiotensin II Receptor Blocker Azilsartan Study for Stronger Blood Pressure Lowering . Phase4

    Clinical Trial
    Molecular Weight

    456.45

    Formula

    C₂₅H₂₀N₄O₅

    CAS No.

    147403-03-0

    SMILES

    O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C(N5)=NOC5=O)C=C3)=CC=C1)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (54.77 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1908 mL 10.9541 mL 21.9082 mL
    5 mM 0.4382 mL 2.1908 mL 4.3816 mL
    10 mM 0.2191 mL 1.0954 mL 2.1908 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    AzilsartanTAK-536TAK536TAK 536Angiotensin ReceptorInhibitorinhibitorinhibit

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    Product Name:
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