Azilsartan

SKU: orb1226207

Description

A specific and potent angiotensin II type 1 receptor (AT1) antagonist with IC50 of 2.6 nM, used in the treatment of adults with essential hypertension. Hypertension Approved(In Vitro):Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells.Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells.Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50 of 2.6 nM.Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation.Azilsartan enhances adipogenesis and exerted greater effects than Valsartan (HY-18204) on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin.(In Vivo):Azilsartan (0-3 mg/kg, Oral gavage, once daily for 5 days) decreases SBP (systolic blood pressure) in obese Koletsky rats at 2 mg/kg.Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration.Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury.

Key Properties

• CAS Number: 147403-03-0
• MW: 456.4501
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₀N₄O₅
• SMILES: CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NC(=O)ON1
• Target: Angiotensin Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Azilsartan (0-3 mg/kg, Oral gavage, once daily for 5 days) decreases SBP (systolic blood pressure) in obese Koletsky rats at 2 mg/kg. Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration. Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury. Animal model: Male Wistar-Kyoto (WKY) rats, obese Koletsky rats (n = 6 per group). Dosage: 0, 1, 2 and 3 mg/kg. Administration: Oral gavage, once daily (9: 00-10: 00 hours) for 5 days. Result: Decreased SBP (systolic blood pressure) in obese Koletsky rats to that of normal rats at 2 mg/kg, whereas the 3 mg/kg dose elicited hypotension. Animal model: Obese Koletsky rats (16, n = 8 per group). Dosage: 0 and 2 mg/kg. Administration: Oral gavage, once daily (9: 00-10: 00 hours) for 21 days. Result: Lowered 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. Animal model: Male Wistar Rats (240–280 g). Dosage: 0, 2, and 4 mg/kg. Administration: Orally, daily for 9 days, starting 7 days before the day of surgery. Result: Individual treatments with Azilsartan (2 & 4 mg/kg) and Coenzyme Q10 (HY-N0111) (20 & 40 mg/kg) significantly attenuated the reduction in locomotor activity. Further, combination treatment with azilsartan (2 mg/kg) and Coenzyme Q10 (20 mg/kg) significantly improved the locomotor activity of animals as compared to their effects per se in BCCAO treated animals.
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• In Vitro:
  Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells. Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells. Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50 of 2.6 nM. Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation. Azilsartan enhances adipogenesis and exerted greater effects than Valsartan (HY-18204) on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. Cell Proliferation Assay Cell line: HepG2 and KDR cells. Concentration: 5, 25, 50, 100 and 200 μM. Incubation time: 24, 48, and 72 h. Result: Gradually decreased the viability of HepG2 cells by increasing the incubation time and dose, the inhibitory concentration of Azilsartan (IC 50%) against HepG2 cells was 100 μM for 24 h treatment time point while in KDR epithelial normal cells no significant cytotoxic effect was observed during the similar treatment conditions. Apoptosis Analysis Cell line: HepG2 cells. Concentration: 100 μM. Incubation time: 24 h. Result: Induced 57.2% early and 0.52% late apoptosis respectively after 24 h.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK-536

Quick Database Links

Gene Symbol

Angiotensin Receptor