Azilsartan|147403-03-0|(阿齐沙坦; TAK-536)-陌孚医药/Medlife

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Azilsartan (Synonyms: 阿齐沙坦; TAK-536)

目录号: PL10952 纯度: ≥99%

CAS No. :147403-03-0

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中文名称	Azilsartan
中文别名	阿齐沙坦;2-乙氧基-1-[[2'-(4,5-二氢-5-氧代-1,2,4-恶二唑-3-基)联苯-4-基]甲基]苯并咪唑-7-羧酸;2-乙氧基-3-((2'-(5-氧代-2,5-二氢-1,2,4-噁二唑-3-基)联苯-4-基)甲基)-3H-苯并[D]咪唑-4-甲酸;阿奇沙坦;阿齐沙坦(阿齐主链);阿齐沙坦酯AZILSARTAN(WITH4INTS.);阿齐沙坦AZILSARTAN;2-乙氧基-1-[[2'-(甲酰胺基)联苯-4-基]甲基]苯并咪唑-7-羧酸甲酯;5-氧代吡咯烷-3-甲酰胺;Azilsartan 阿齐沙坦;Azilsartan 抑制剂;阿齐沙坦标准品;阿齐沙坦原药;阿齐沙坦杂质;阿齐沙坦杂质对照品;阿齐沙坦酯;角鲨烯;原药阿齐沙坦;克林霉素;阿齐沙坦酯杂质A;阿齐沙坦(降压药);阿齐沙坦INT E;阿齐沙坦原料药;阿奇沙坦 10G
英文名称	Azilsartan
英文别名	Azilsartan;2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid;Tak 536;Unii-F9nux55p23;2-ethoxy-3-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)Methyl)-3H-benzo[d]iMidazole-4-carboxylic acid;Azilsartan 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]Methyl]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-1H-benziMidazole-7-carboxylic Acid;Azilsartan (TAK-536);2-ethoxy-3-[[4-[2-(5-oxo-2H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid;zilsartan;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;TAK-536;AZATMint-E;Azilsartan API;Azilsartan metabolite MI D4;Azilsartan metabolite MII-D4;AzilsartanMedoxoMilInterMediates-3;F9NUX55P23;2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid;AK121790;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-;2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-ox
Cas No.	147403-03-0
分子式	C₂₅H₂₀N₄O₅
分子量	456.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 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.

性状

Solid

体外研究(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 I-Sar-Ile-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. has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Kajiya T, et al. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83.
[2]. Zhao M, et al. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats. Diabetes Obes Metab. 2011 Dec;13(12):1123-9.

溶解度数据	In Vitro: DMSO : 25 mg/mL (54.77 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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