Azilsartan

SKU: orb1309918

Description

Azilsartan (TAK-536) is a selective angiotensin II type 1 receptor antagonist used in research to study hypertension mechanisms. It is applied in both in vitro binding assays and in vivo models to investigate cardiovascular physiology and the renin-angiotensin system pathway.

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 147403-03-0
• MW: 456.4501
• Purity: 99.87% (May vary between batches)
• Formula: C₂₅H₂₀N₄O₅
• SMILES: CCOC1=NC2=C(N1CC1=CC=C(C=C1)C1=C(C=CC=C1)C1=NC(=O)ON1)C(=CC=C2)C(O)=O
• Target: RAAS,Reactive Oxygen Species,ROS,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.38 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (120.5 mM)

Bioactivity

• Target IC50:
  AT1 receptor:2.6 nM
• In Vivo:
  In 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.
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• In Vitro:
  Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors. 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. In isolated rabbit aortic strips, Azilsartan reduces the maximal contractile response to AII with a pD'2 value of 9.9. The inhibitory effects of Azilsartan on contractile responses induced by AII persists after the strips are washed. Azilsartan suppresses the increase in plasma glucose level in the oral glucose tolerance test (OGTT) without significant change in insulin concentration and improved insulin sensitivity. In skeletal muscle, Azilsartan decreases the expression of TNF-α at doses of 0.001%. In adipose tissue, Azilsartan reduces TNF-α expression but increases the expression of adiponectin, PPARγ, C/EBα, and aP2. In cultured 3T3-L1 preadipocytes, Azilsartan enhances adipogenesis and exertes greater effects than valsartan on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. Azilsartan also potently inhibits vascular cell proliferation in the absence of exogenously supplemented angiotensin II.
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• Cell Research:
  Twenty-four hours after transfections, the COS-7 cells expressing human AT1 receptors 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 Azilsartan 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 AII 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 Azilsartan before stimulation with AII. The accumulation of inositol 1-phosphate (IP1) is measured by using an IP-One Tb kit. The fluorescence resonance energy transfer signal is measured on a plate reader.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KDR cells, inhibit, Ischemia, Neuroprotection, endothelial, Inhibitor, Hypertension, HepG2, adipogenesis, Angiotensin Receptor, Apoptosis, AT1 receptor, Azilsartan, cancer, Stroke, TAK 536, TAK536, TAK-536, Reactive Oxygen Species, vascular cell

Compound Identifiers

PubChem CID

135415867