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- 详细信息
- 文献和实验
- 技术资料
- 英文名:
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
- 供应商:
上海安毕达生物科技有限公司
- CAS号:
863031-21-4
- 规格:
50μL/1mL/1mg/5mg/10mg/50mg/100mg
| 规格: | 50μL | 产品价格: | ¥149.0 |
|---|---|---|---|
| 规格: | 1mL | 产品价格: | ¥876.0 |
| 规格: | 1mg | 产品价格: | ¥250.0 |
| 规格: | 5mg | 产品价格: | ¥630.0 |
| 规格: | 10mg | 产品价格: | ¥945.0 |
| 规格: | 50mg | 产品价格: | ¥2800.0 |
| 规格: | 100mg | 产品价格: | ¥3920.0 |
Azilsartan Medoxomil, a new angiotensin II Type 1 receptor blockers with IC50 of 0.62 nM. In conscious spontaneously hypertensive rats (SHRs), oral administration of 0.1-1mg/kg azilsartan medoxomil significantly reduced blood pressure at all doses even 24h after dosing3. Azilsartan medoxomil, in 40 and 80 mg doses, combined with 5 mg of the calcium channel blocker amlodipine was well tolerated and led to meaningful additional BP(blood pressure) reductions compared with placebo plus amlodipine4. Further, in aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1(angiotensin II type 1) receptors5.
溶解方案(细胞实验)
DMSO 中的溶解度 : 125 mg/mL (219.87 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)
溶解方案(动物实验)
"方案 一": "请依序添加每种溶剂:10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.08 mg/mL (3.66 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。"
"方案 二": "请依序添加每种溶剂:10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (3.66 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。"
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文献和实验Ojima M, Igata H, et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8.
Kusumoto K, Igata H, Ojima M, Tsuboi A, Imanishi M, Yamaguchi F, Sakamoto H, Kuroita T, Kawaguchi N, Nishigaki N, Nagaya H. Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models. Eur J Pharmacol. 2011 Nov 1;669(1-3):84-93. doi: 10.1016/j.ejphar.2011.07.014. Epub 2011 Jul 28. PMID: 21816148.
Weber MA, White WB, Sica D, Bakris GL, Cao C, Roberts A, Kupfer S. Effects of combining azilsartan medoxomil with amlodipine in patients with stage 2 hypertension. Blood Press Monit. 2014 Apr;19(2):90-7. doi: 10.1097/MBP.0000000000000027. PMID: 24445723; PMCID: PMC3966914.
Kajiya T, Ho C, Wang J, Vilardi R, Kurtz TW. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83. doi: 10.1097/HJH.0b013e32834c46fd. PMID: 21986624.
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