产品
编 号：F171583
分子式：C25H20N4O5
分子量：456.45
分子式：C25H20N4O5
分子量：456.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
10mg
240
In-stock
25mg
480
In-stock
50mg
720
In-stock
100mg
1200
In-stock
结构图
CAS No: 147403-03-0
产品详情
生物活性：
Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.
体内研究：
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.
体外研究：
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.
Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.
体内研究：
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.
体外研究：
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.
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