Azilsartan

Research use only, not for human use.

A specific and potent angiotensin II type 1 receptor (AT1) antagonist with IC50 of 2.6 nM.

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.

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.

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.

TAK-536

GPCR/G Protein

Angiotensin Receptor

AT1receptor

Cardiovascular Disease

Hypertension

147403-03-0

456.4501

C25H20N4O5

>98% (HPLC)

10 mM in DMSO

CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NC(=O)ON1

1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-

(-20℃)

With Ice Pack

≥ 2 years