Azilsartan (TAK-536) 是一种口服有效的、选择性和特异性的血管紧张素 Ⅱ 1 型受体 (AT1) 拮抗剂。Azilsartan 诱导 HepG2 细胞ROS形成和细胞凋亡 (apoptosis)。Azilsartan 具有神经保护和抗癌活性。Azilsartan 可以用于高血压和中风研究。
| 生物活性 | Azilsartan (TAK-536) is an orally active, potent, selective and specificangiotensin II type 1 receptor (AT1)antagonist. Azilsartan inducesROSformation andapoptosisin HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[1][2][3][4][5]. |
体外研究
(In Vitro) | Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells[5].
Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells[5].
Azilsartan inhibits the specific binding of125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50of 2.6 nM[3].
Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation[5].
Azilsartan enhances adipogenesis and exerted greater effects thanValsartan(HY-18204) on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin[1].
Cell Proliferation Assay[5] | 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[5] | 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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体内研究
(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[2].
Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration[2].
Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury[4].
| Animal Model: | Male Wistar-Kyoto (WKY) rats, obese Koletsky rats (n=6 per group)[2] | | 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)[2] | | 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)[4] | | 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) andCoenzyme 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(54.77 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 2.5 mg/mL (5.48 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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