| CAS |
No.124750-99-8 |
| 中文名称 |
氯沙坦钾(10mM in DMSO,无菌） |
| 英文名称 |
Losartan Potassium(10mM in DMSO，Sterile） |
| 分子式 |
C22H22CIKN6O |
| 分子量 |
461 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Angiotensin Receptor（AT） |
| 通路 |
GPCR & G Protein |
| 背景说明 |
是血管紧张素II受体1型 (AT1)拮抗剂。 |
| 生物活性 |
Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist， competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.[1-5] |
| In Vitro |
Losartan potassium 竞争血管紧张素 II 与 AT1 受体的结合。抑制 50% 血管紧张素 II 结合的浓度 (IC50) 为 20 nM[1]。Losartan potassium (40 μM) 影响 ISC 但阻止 ANGII 对 ISC 的影响[2]。Losartan potassium 显著降低子宫内膜癌细胞中 Ang II 介导的细胞增殖。与单独使用每种药物相比，Losartan potassium 和抗 miR-155 的组合具有显著更强的抗增殖作用[3]。 |
| In Vivo |
Losartan potassium (0.6 g/L，po) 处理的 Fbn1C1039G/+ 小鼠显示相对于安慰剂处理的 Fbn1C1039G 远端空域口径减少/+ 。滴定 Losartan potassium 和普萘洛尔的剂量以达到可比较的血液动力学效果。pSmad2 核染色分析表明，Losartan potassium 拮抗 Fbn1C1039G/+ 小鼠主动脉壁中的 TGF-β 信号传导。Losartan potassium 可以改善肺部的疾病表现，这一事件与改善的血流动力学似乎无关[4]。Losartan potassium (10 mg/kg，动脉内注射) 使血液血管紧张素水平增加四到六倍。Losartan potassium (10 mg/kg，ip) 使血浆肾素水平增加 100 倍；血浆血管紧张素原水平降至对照的 24%；和血浆醛固酮水平没有变化[5]。 |
| 细胞实验 |
An MTT assay is used to measure cell proliferation and viability. For the assay， 5000 cells in 200?μL media per well are seeded in a 96 well plate. After overnight incubation to allow for cell attachment， the medium is removed by suction. MTT at 1?mg/mL concentration in serum-free medium is added and then incubated for 4?h at 37°C. After removal of MTT solution， 100?μL of DMSO is added to dissolve formazan crystals. Absorbance at 570?nm and at 600?nm as a reference is then measured using a microplate reader. The difference in absorbance is thus relative to the extent of cell survival. |
| 动物实验 |
Female Fbn1C1039G/+ mice undergo timed matings with wild-type male mice. At 14.5d post-coitum， pregnant female Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=10)， propranolol (0.5 g/L; n=6) or placebo (n=12). Therapy is continued throughout lactation and after weaning until 10 months of age. Mice are sacrificed and examined using the techniques described above. Propranolol is used for comparison with losartan because β-adrenergic receptor blockade is the current albeit controversial standard of care to modulate abnormal growth of the aortic root in MFS. Beginning at 7 weeks of age， wild-type and Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=5)， propranolol (0.5 g/L; n=7) or placebo (n=10). Mice are continued on oral therapy for 6 months and then sacrificed. |
| 数据来源文献 |
[1]. Burnier， M. Angiotensin II type 1 receptor blockers. Circulation， 2001. 103(6): p. 904-12.
[2]. Ashry， O.， et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol， 2014.
[3]. Choi， C.H.， et al. Angiotensin II type I receptor and miR-155 in endometrial cancers: synergistic antiproliferative effects of anti-miR-155 and losartan on endometrial cancer cells. Gynecol Oncol， 2012. 126(1): p. 124-31.
[4]. Habashi， J.P.， et al. Losartan， an AT1 antagonist， prevents aortic aneurysm in a mouse model of Marfan syndrome. Science， 2006. 312(5770): p. 117-21.
[5]. Campbell， D.J.， et al. Effects of losartan on angiotensin and bradykinin peptides and angiotensin-converting enzyme. J Cardiovasc Pharmacol， 1995. 26(2): p. 233-40. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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