氯沙坦 T0215L

Product Introduction
Bioactivity


英文名: Losartan

描述: Losartan (DuP-753) 是一种血管紧张素II 受体拮抗剂，能够与血管紧张素II 竞争性结合AT1受体(IC50:20 nM)。

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.

体外活性: Losartan 与血管紧张素II竞争性地结合AT1受体。其抑制血管紧张素II结合50%所需浓度（IC50）为20 nM[1]。Losartan （40μM）影响ISC，但可阻止ANGII对ISC的作用[2]。Losartan 显著降低血管紧张素II介导的子宫内膜癌细胞增殖。Losartan 与抗miR-155联合使用，相比单药治疗具有更显著的抑制增殖效果[3]。

体内活性: 与安慰剂处理的 Fbn1C1039 g/+ 小鼠相比，Losartan （0.6 g/L，p.o.）处理的 Fbn1C1039 g/+ 小鼠显示出远端气室口径的缩小。Losartan 和普萘洛尔的剂量经过滴定，可产生血液动力学效应。对 pSmad2 核染色的分析表明，Losartan 能拮抗 Fbn1C1039 g/+ 小鼠主动脉壁的 TGF-β 信号传导。Losartan 能改善肺部的疾病表现，但这与血液动力学的改善并无必然联系[4]。Losartan （10 mg/kg，动脉内注射）可使血液中的血管紧张素水平增加 4 到 6 倍。Losartan （10 mg/kg，静脉注射）可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组的 24%，血浆醛固酮水平保持不变[5]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (106.41 mM)


关键字: DuP 753 | Angiotensin Receptor | DuP753 | Losartan | inhibit | Inhibitor

相关产品: Fimasartan | Novokinin acetate | L162389 | SSAA09E2 | Lisinopril | Irbesartan | VTP-27999 TFA | Aliskiren D6 hemifumarate | Remodelin hydrobromide | H-Val-Pro-Pro-OH

相关库: Drug Repurposing Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | Endocrinology-Hormone Compound Library

氯沙坦 T0215L信息由TargetMol中国为您提供，如您想了解更多关于氯沙坦 T0215L报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途